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Physiol Rev
84: 699 –730, 2004; 10.1152/physrev.00033.2003.
Phosphoinositides in Constitutive Membrane Traffic
MICHAEL G. ROTH
Department of Biochemistry, University of Texas Southwestern Medical Center at Dallas, Dallas, Texas
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I. Introduction
II. Enzymes That Modify Phosphoinositides Are Important for Membrane Traffic
A. PI 3-kinases and PtdIns 3-kinases
B. PtdIns 4-kinases
C. PIP 5-kinases
D. PIP 4-kinases
E. Phosphatases acting on phosphoinositides
III. Phosphoinositide-Binding Modules That Function in Constitutive Membrane Traffic
A. PH domains
B. PX domains
C. FYVE domains
D. ENTH/ANTH domains
E. Basic sequences and other motifs that bind phosphoinositides
IV. Intracellular Distribution and Function of Phosphoinositides for Membrane Traffic
A. PtdIns(4,5)P2 at the plasma membrane
B. PtdIns(3)P on endosomes
C. PtdIns(3,5)P2 on MVEs/vacuoles
D. PtdIns(3)P on the Golgi
E. PtdIns(4)P and PtdIns(4,5)P2 on the Golgi
F. Phosphoinositides on the ER
V. Summary and Conclusions
Roth, Michael G. Phosphoinositides in Constitutive Membrane Traffic. Physiol Rev 84: 699 –730, 2004; 10.1152/
physrev.00033.2003.—Proteins that make, consume, and bind to phosphoinositides are important for constitutive membrane traffic. Different phosphoinositides are concentrated in different parts of the central vacuolar pathway, with
phosphatidylinositol 4-phosphate predominate on Golgi, phosphatidylinositol 4,5-bisphosphate predominate at the
plasma membrane, phosphatidylinositol 3-phosphate the major phosphoinositide on early endosomes, and phosphatidylinositol 3,5-bisphosphate found on late endocytic organelles. This spatial segregation may be the mechanism by which the
direction of membrane traffic is controlled. Phosphoinositides increase the affinity of membranes for peripheral membrane proteins that function for sorting protein cargo or for the docking and fusion of transport vesicles. This implies that
constitutive membrane traffic may be regulated by the mechanisms that control the activity of the enzymes that produce
and consume phosphoinositides. Although the lipid kinases and phosphatases that function in constitutive membrane
traffic are beginning to be identified, their regulation is poorly understood.
I. INTRODUCTION
The organelles of the secretory and endocytic pathways in eukaryotic cells have distinct functions, molecular composition, and luminal environment. To achieve
this diversity of structure and purpose, the membranes of
these organelles must be kept separate for the most part,
or they would rapidly fuse and become homogeneous (98,
263). Constitutive membrane traffic is the process by
which membrane lipids, integral membrane proteins, and
the soluble protein content of membrane organelles are
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moved from the endoplasmic reticulum (ER) where they
are synthesized to the sites where they function. This
process requires collecting proteins and lipids that should
move from those that should remain behind and packaging them into a transport intermediate (usually thought of
as a small vesicle, but this might not be the case in every
instance). The transport intermediate fissions from its
source membrane and is actively moved to its destination
membrane where it fuses and delivers cargo. The process
of forming transport intermediates is now understood in
some detail (331). Constitutive membrane traffic is very
0031-9333/04 $15.00 Copyright © 2004 the American Physiological Society
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MICHAEL G. ROTH
1
In this review phosphatidylinositol is abbreviated PtdIns. The
phosphorylated phosphatidylinositols are referred to as phosphoinositides, abbreviated as PIPs. Kinases that can act on either PtdIns or PIP
are abbreviated as PIXK, where X refers to the position on the inositol
head group that is modified. Kinases that act only on PIPs and not PtdIns
are referred to as PIPXK. Kinases that only phosphorylate PtdIns are
abbreviated as PtdInsXK.
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Currently there are abundant data indicating that
phosphatidylinositol 3-phosphate [PtdIns(3)P], phosphatidylinositol 4-phosphate [PtdIns(4)P], phosphatidylinositol 3,5-bisphosphate [PtdIns(3,5)P2], and phosphatidylinositol 4,5-bisphosphate [PtdIns(4,5)P2] play important roles
in constitutive membrane traffic. However, the number
and diversity of roles that any lipid plays in any step in
membrane traffic are not yet known precisely. Proteins
known to be essential for membrane traffic bind to PIPs at
defined locations in the cell, suggesting that one of the
functions of these lipids is to establish membrane identity. The activity of some proteins is modified when they
bind a particular PIP, indicating that these lipids can act
as allosteric regulators. PIPs are also generated and consumed at locations where lipid bilayers are being sharply
curved in the processes of membrane fission and fusion. It
has been proposed that the changes in lipid shape that
occur as PIPs are phosphorylated or dephosphorylated
contribute to this process (43). To complicate matters,
PIP species can be interconverted by kinases and phosphatases and can even act as regulators of their own
production. Determining which, if any, of these processes
is important for a particular step in membrane traffic has
been a challenge. In addition, PIPs affect the membrane
activity of a number of proteins that may have no direct
impact on membrane traffic but are found on the organelles where membrane traffic occurs. There currently
is little understanding of how potentially mobile lipids
such as PIPs can be restricted to membrane subdomains
or how competition among various cytosolic PIP-binding
proteins is controlled.
Most of our current knowledge of the role of PIPs in
constitutive membrane traffic is based on experiments that
show that a particular enzyme activity is required (directly
or indirectly) for a specific step in membrane traffic or on
the discovery that a protein implicated as functioning in
membrane traffic can bind PIPs. Relatively less is known
about how the lipids themselves function in this process.
Thus I will begin by summarizing what is known about the
role in constitutive membrane traffic for enzymes that modify PIPs followed by a summary of the proteins known to be
involved in membrane traffic that bind each lipid. I will
summarize what is known about the distribution of PIPs in
cells and finish with more speculative comments on the
possible roles of the lipids. I will borrow concepts from our
understanding of signal transduction processes to propose a
hypothesis to explain how local production of PIPs might
contribute to the generation of a transient membrane microdomain and how this might function in the process of
constitutive membrane transport.
Superimposed on constitutive membrane traffic are
many examples of regulated membrane transport in which
PIPs probably serve multiple functions in both membrane
traffic and signal transduction. The task of separating direct
functions of PIPs in membrane traffic from indirect conse-
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active, and in mammalian cells, many membrane proteins
constantly cycle through multiple organelles on a time
scale of tens of minutes. In addition to this continual
traffic, there are many instances where the rates and
direction of movement of membrane proteins and lipids
are rapidly changed in response to signals from the extracellular environment. This “regulated” membrane traffic uses much the same machinery and principles as constitutive traffic. The history of research into the mechanisms of constitutive membrane traffic is that of continual
discovery of unexpected levels of complexity and regulation (228). There are many more proteins that function for
any one step in membrane traffic and many more levels of
regulation than we would have thought necessary. In this
aspect, research into membrane traffic resembles research into mechanisms of signal transduction. This is
more than coincidence. Membrane traffic is controlled
through intracellular signal transduction mechanisms that
probably work by the same general principles as those
that regulate gene expression in response to environmental cues.
Phosphoinositides were first recognized to be important as intermediates in signal transduction cascades
where they serve as second messengers and signal integrators. Subsequently mutations that interfered with
membrane traffic were mapped to genes encoding kinases
and phosphatases that act on phosphatidylinositol
(PtdIns) and phosphoinositides (the phosphorylated derivatives of PtdIns), and the role that these lipids play in
membrane traffic began to be appreciated (reviewed in
Refs. 53, 64, 66, 70, 74, 217, 219, 294, 295).1 Phosphoinositides (PIPs) are found in unicellular organisms and
thus must have appeared quite early in evolutionary history. Whether the phosphorylation of PtdIns to multiple
species first arose as part of a mechanism by which cells
sensed their external environment, or as part of the machinery for moving membrane proteins between compartments, the molecular strategies for their use are probably
similar. Thus it is likely that in membrane traffic PIPs
contribute to a complex web of feedback pathways that
generate a combinatorial control mechanism, just as they
do in signal transduction. This ensures that actions such
as vesicle budding or fusion do not occur unless multiple
conditions are satisfied, and vesicles do not normally
form unless they contain cargo and do not fuse unless
they have reached the correct destination.
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PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
II. ENZYMES THAT MODIFY
PHOSPHOINOSITIDES ARE IMPORTANT
FOR MEMBRANE TRAFFIC
A. PI 3-Kinases and PtdIns 3-Kinases
Although it has been appreciated for 50 years that
secretion stimulated by hormones is accompanied by
changes in intracellular PIP pools (147), the realization
that PIPs were also important for constitutive membrane
TABLE
1.
traffic arose when a mammalian PI 3-kinase was cloned
(140, 312) and found to have strong sequence homology to
Vps34p, a yeast protein known to be essential for the
delivery of proteins to the vacuole in Saccharomyces
cerevisiae (137, 334). Subsequently, the PI 3-kinase inhibitor wortmannin was discovered to affect multiple steps
in membrane traffic (reviewed in Refs. 36, 295). Although
wortmannin inhibits multiple enzymes (68, 250, 253),
complicating the interpretation of many experiments, its
use pointed the way to more sophisticated investigations
employing forward and reverse genetics. It is now clear
that a number of enzymes that modify PIPs are required
for constitutive membrane traffic and that others probably influence membrane traffic indirectly by modifying the
actin cytoskeleton (Table 1). Most recently, some enzymes that participate in signal transduction events have
been discovered to also participate in the rapid removal of
hormone receptors by endocytosis.
The kinases that phosphorylate PtdIns or PIPs on the
D-3 position can be organized into three classes according
to amino acid sequence relationships (82, 106). Although
class I PI3Ks can phosphorylate PtdIns, PtdIns(4)P,
Properties of PtdIns and PIP kinases that function in membrane traffic
Location
Species
Molecular
Weight
Golgi, endosomes
Golgi, endosomes
Clathrin-coated
pits
Mammalian
Saccharomyces cerevisiae
Mammalian
Golgi
Nucleus, Golgi
Golgi, synapse
PM, ER, Golgi
?
Enzyme
Substrate
Product
101
101
170
PtdIns
PtdIns
PtdIns,
PtdIns(4)P
PtdIns(4,5)P2
PtdIns(3)P
PtdIns(3)P
PtdIns(3)P
PtdIns(3,4)P2
PtdIns(3,4,5)P3
106, 367
313, 333
80, 81
Mammalian
S. cerevisiae
Mammalian
Mammalian
S. cerevisiae
90
125
55
55
55
PtdIns
PtdIns
PtdIns
PtdIns
PtdIns
PtdIns(4)P
PtdIns(4)P
PtdIns(4)P
PtdIns(4)P
PtdIns(4)P
12, 86, 120, 233, 392
102, 113
17, 123, 237
17, 372, 377
130, 315
PM
Mammalian
61
PM
Mammalian
61
PIP5KC
Synapse
Mammalian
87, 90
Mss4
Nucleus, PM
S. cerevisiae
89
PIKfyve
Late endosomes
Mammalian
235
Fab1p
Vacuole
S. cerevisiae
257
PtdIns(5)P
PtdIns(4,5)P2
PtdIns(3,5)P2
PtdIns(3,4,5)P3
PtdIns(5)P
PtdIns(4,5)P2
PtdIns(3,5)P2
PtdIns(3,4,5)P3
PtdIns(4,5)P2
PtdIns(3,5)P2
PtdIns(3,4,5)P3
PtdIns(4,5)P2
PtdIns(3,4)P2
PtdIns(5)P,
PtdIns(3,5)P2
PtdIns(3,5)P2
157, 209, 357
PIP5KB
PtdIns
PtdIns(4)P,
PtdIns(3)P,
PtdIns(3,4)P2
PtdIns
PtdIns(4)P,
PtdIns(3)P,
PtdIns(3,4)P2
PtdIns(4)P,
PtdIns(3)P,
PtdIns(3,4)P2
PtdIns(4)P,
PtdIns(3)P
PtdIns,
PtdIns(3)P
PtdIns(3)P
3-Kinases
PtdIns3KIII
VPS34p
PtdIns3KIIC2␣
4-Kinases
PtdIns4KIII␤
Pik1
PtdIns4KII␣
PtdIns4KII␤
LSB6/PIK2
5-Kinases
PIP5KA
Reference Nos.
157, 209, 357
158, 382
8, 75, 76, 150
156, 306, 308, 319
5, 115, 258, 399
PM, plasma membrane; ER, endoplasmic reticulum; PtdIns, phosphatidylinositol; P, phosphate; P2, bisphosphate; P3, trisphosphate.
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quences of downstream signaling cascades is exceedingly
difficult. For example, there is an extensive and interesting
literature on the effects on membrane traffic that occur
when peptide hormone or growth factor receptors activate
phosphatidylinositol 3-kinases (63, 71), but it is still unclear
if the lipid products of the hormone-activated 3-kinases have
a direct effect on endocytosis. For the sake of simplicity, this
review is focused on the discussion of aspects of membrane
traffic not acutely controlled by extracellular signals. In
addition, many genetic studies have identified mutations in
proteins that make or bind to phosphoinositides that impact
membrane traffic, as well as having pleotropic effects on
cytoskeleton or other aspects of cell metabolism. Many of
the proteins are undoubtedly interesting, but this review is
limited to those for which there is some evidence that they
directly affect membrane traffic.
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MICHAEL G. ROTH
1. PtdIns3K and Vps34p
Vps34p associates with a serine/threonine protein
kinase, Vps15p, as a heterodimer (334). Binding to Vps15p
is required for Vps34p to associate with membranes. Human PtdIns3K binds a 150-kDa homolog of Vps15p and in
this heterodimeric form associates with, and is activated
by, phosphatidylinositol transfer protein (PITP) (264).
PITP plays a role in a number of different membrane
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traffic events (52, 179), perhaps by transferring substrates
to the kinases. Vps34p was first identified as a protein
required for the sorting of vacuolar enzymes into the
pathway leading from the Golgi to the vacuole in S. cerevisiae (137, 312, 334). It was assumed that the site of
action of the enzyme was at the Golgi, since in the absence of Vps34p vacuolar proteins were not sorted correctly and were secreted. Additional evidence supporting
a Golgi location for Vps34p/PtdIns3K was provided by
treating mammalian cells with wortmannin. Wortmannin
inhibited the delivery of cathepsin D to lysosomes (28, 72)
apparently through an effect on the sorting of cargo into
vesicles rather than through an inhibition of vesicle budding. Wortmannin had only a minor effect on the production of small vesicles from trans-Golgi network (TGN)
membranes but prevented the mannose 6-phosphate receptor from entering into vesicles (110). However, yeast
Vps34p or mammalian PtdIns3K have not been shown to
be located on Golgi or TGN membranes. As is described
in more detail below, the proteins that have been discovered to bind PtdIns(3)P are all located on endocytic membranes. In fact, the phenotypes observed when PtdIns3K
activity is inhibited do not require that the enzyme act at
the TGN. If PtdIns(3)P generated on endosomes was necessary for the recycling of sorting receptors from endosomes to the Golgi, then loss of PtdIns3K function would
cause the observed phenotypes at the Golgi as the sorting
receptors became trapped in endosomes.
2. PtdIns3KIIC2␣
PtdIns3KIIC2␣ has recently been reported to localize
in clathrin-coated structures at the plasma membrane and
TGN (80, 112). This enzyme binds to clathrin through
amino-terminal sequences, and this derepresses enzymatic activity (112). Overexpression of PtdIns3KIIC2␣ in
COS cells inhibited internalization of transferrin receptors and prevented accumulation of mannose 6-phosphate
receptors in the TGN, presumably by inhibiting the uncoating of clathrin-coated vesicles (112). Previously, it
was observed that PtdIns(3)P and, to a lesser extent,
PtdIns(3,4)P2 enhanced the binding of AP2 adaptors to
peptides containing internalization signals. Clathrin binding enhanced the affinity of AP2 for internalization signals
to a similar extent, but the effect of clathrin and
PtdIns(3)P were not additive (286). However, when fluorescent proteins that bind PtdIns(3)P are expressed in
cells, they label endosomes and not the plasma membrane
(32, 92, 318), suggesting that there is little free PtdIns(3)P
at the cell surface. There is a recent report that
PtdIns3KIIC2␣ localizes to the nucleus rather than the
plasma membrane (77). More work is required to determine how PtdIns3KIIC2␣ functions in membrane traffic
and to what extent PtdIns(3)P is involved in membrane
traffic from the plasma membrane.
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PtdIns(5)P, and PtdIns(4,5)P2 in vitro, agonists that stimulate their activity mainly generate PtdIns(3,4)P2 and
phosphatidylinositol 3,4,5-trisphosphate [PtdIns(3,4,5)P3],
two lipids present in very low amounts in quiescent cells.
Thus the class I enzymes probably phosphorylate mainly
PtdIns(4)P and PtdIns(4,5)P2 in vivo and are important
for signal transduction. Upon activation, platelet-derived
growth factor (PDGF) receptors bind PI3KI enzymes.
Both PI3KI binding and enzyme activity are required to
sort the receptors into the degradative pathway after
internalization (165). However, it is not clear whether
this is a downstream effect of signaling through
PtdIns(3,4,5)P3 produced at the plasma membrane or a
consequence of generating PIPs on endosomes. Low concentrations of wortmannin and LY294002 inhibit the endocytic traffic of transferrin receptors (220, 321, 329).
Because these concentrations of inhibitors inhibit PI3KIs
but not the yeast Vps34p, it was proposed that a class I
enzyme might be involved in endocytosis. However, mammalian PI3KIII is inhibited by wortmannin at low nanomolar concentrations (367) and probably was responsible
for some of the effects observed. PI3KI isoforms bind to
regulatory subunits, and one of these, p85␣, was identified
as part of a protein complex required for the budding of
vesicles containing the polyimmunoglobulin receptor
from isolated Golgi membranes (170). This budding reaction was inhibited by micromolar wortmannin, a concentration much higher than required to inhibit known class
I PI3Ks, and more consistent with inhibition of PI3KII.
The identity of the PI3K that might interact with p85␣ on
the Golgi is currently unknown. Thus there is currently no
clear evidence for a direct role of PI3KI enzymes in constitutive membrane traffic.
Class II PI3Ks can phosphorylate PtdIns, PtdIns(4)P,
and PtdIns(4,5)P2 in vitro. Relatively little is known about
the lipids that class II enzymes produce in vivo. However,
PtdIns3KIIC2␣ is found in clathrin-coated pits at the
plasma membrane and on the Golgi (80) and may play a
role in membrane traffic (112). The majority of PtdIns(3)P
in mammalian cells is produced by class III PI3K (363),
the mammalian counterpart of Vps34p (367). PI3KIII
phosphorylates only PtdIns to PtdIns(3)P and is more
properly called PtdIns3K. This enzyme is required for
membrane traffic in the endocytic pathway and probably
does not play a role in signal transduction.
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
B. PtdIns 4-Kinases
1. PtdIns4KIII␤/PIK1
Pik1p is an essential 125-kDa enzyme of S. cerevisiae
(102) found both in the nucleus and on Golgi membranes
(370). The phenotype of pik1ts yeast grown at nonpermissive temperature is similar to the phenotype produced by
a conditional loss of ARF function (9). Overexpression of
Pik1p suppresses the defect in secretion in yeast expressing a temperature-sensitive allele of Sec14, the yeast PITP
(129). The mammalian Pik1p counterpart, PtdIns4KIII␤, is
a 90-kDa enzyme that has been localized to Golgi membranes (120, 392). PtdIns4KIII␤ enzyme activity is stimulated in vitro by ARF1 (120), suggesting that it is an
effector of ARF for membrane traffic. Overexpression of
mammalian frequenin, the homolog of an activator of
Pik1p in S. cerevisiae (136), stimulates the delivery of a
reporter protein to the apical surface in polarized cells
(379). Both the PtdIns4KIII␤ and Pik1p behave as soluble
proteins (102, 392), suggesting that their association with
membranes must be dynamic and regulated. PtdIns4KIII␤
is inhibited by 50 –100 nM wortmannin (233), but Pik1p is
highly resistant to this inhibitor.
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PtdIns4K activity is found on chromaffin granules
and on small synaptic vesicles and is required for vesicle
fusion (386, 387). PtdIns4K activity is also found on vesicles containing the Glut4 glucose transporter isolated
from muscle (190). The identity of the enzymes responsible for these activities is not known.
2. PtdIns4KII/PIK2
Biochemical studies indicate that type II PtdIns4K is
responsible for much of the PtdIns 4-kinase activity in
response to extracellular signal transduction (106). There
are two isoforms of the mammalian enzyme (17, 237, 372,
377). PtdIns4KII␣ is located on perinuclear membranes
that include the Golgi and on synaptic membranes (123,
372). Overexpression of PtdIns4KII␣ in fibroblasts has no
effect on transport of a reporter from the ER to the Golgi
but does stimulate transport from the TGN to plasma
membrane (372). Knockout of PtdIns4KII␣ by small interfering RNA oligonucleotides causes AP1 clathrin coats to
be released from Golgi membranes, and the Golgi to
fragment. Export of a viral glycoprotein from the TGN is
also inhibited. The binding of AP1 to Golgi in these cells
can be rescued by replacing PtdIns(4)P but not by replacing PtdIns(4,5)P2. However, the glycoprotein transport
defect is rescued by both lipids. Thus the effect of
PtdIns4KII␣ appears to be to produce PtdIns(4)P, which
is directly recognized by coat proteins at the TGN and
also serves as a precursor of the PtdIns(4,5)P2 required
for membrane transport to the plasma membrane (372).
A PtdIns4KII activity coprecipitates with CD63, a
tetraspannin protein found mainly on lysosomes (50, 231),
and is also found in plasma membrane lipid rafts, although it is not enriched in rafts that contain caveolin (376). The single yeast homolog of mammalian
PtdIns4KIIs is LSB6, now renamed PIK2. This gene is
nonessential (130, 315), indicating that it is not required
for the functioning of the secretory pathway, although it
still might have a more specialized role in secretory processes. The functions of endosomes and the vacuole are
not essential for yeast to grow in the laboratory, so a role
of PIK2 in endocytic processes is still possible.
C. PIP 5-Kinases
PIP 5-kinases were originally purified as activities
that phosphorylated PtdIns(4)P to PtdIns (4,5)P2 and subsequently cDNAs for six enzymes have been cloned (25,
37, 157, 159, 209). Based on sequence relationships, the
PIP5Ks were grouped into two families called types I and
II. Subsequently, it was realized that type II kinases phosphorylated the D-4 position and not D-5 and that both type
I and II enzymes also phosphorylated the D-3 position
(283, 409). Thus the PIP5KII proteins are more accurately
called PIP4Ks. The ␣- and ␤-type I kinases were shown to
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Two distinct classes of kinases phosphorylate PtdIns
at the D-4 position. These are called type II and type III
(type I was discovered to be a PtdIns 3-kinase). Type III
enzymes are homologous to two yeast PtdIns4Ks, PIK1
(102) and STT4 (405). The mammalian ortholog of STT4 is
PtdIns4KIII␣ (251, 391) and the ortholog of PIK1 is
PtdIns4KIII␤ (12, 233, 250). In yeast, STT4 and PIK1 do
not compensate for each other in deletion studies, with
STT4 functioning in regulation of the actin cytoskeleton
and PIK1 essential for membrane traffic (9, 129, 370).
PtdIns4KIII␤ has been localized to the Golgi, a location
consistent with the work on yeast PIK1 (120, 392). STT4
was identified in a screen for mutations in S. cerevisiae
that prevent aminophospholipid transport to the Golgi
(358), and its mammalian counterpart, PtdIns4KIII␣, is
reported to localize at the ER (251). However, currently
there is no evidence that the effect of STT4 on lipid traffic
is direct. By extension, it is possible that mammalian
PtdIns4KIII␣ is not involved in membrane traffic.
Type II PtdIns4K␣ and -␤ were only recently cloned
(17, 237). These enzymes do not have the signature PIK
domain and belong to a family of lipid kinases distinct
from the other PtdIns3/PtdIns4 kinases. PtdIns4KII␣ is a
major contributor to cellular PtdIns(4)P levels and is
located on the Golgi where it plays a role in membrane
traffic from the TGN (372). PtdIns4KII␤ is a cytosolic
protein that is recruited to plasma membrane and activated by Rac1 and may have no role in membrane traffic
(377). In S. cerevisiae, Lsb6p is the ortholog of mammalian PtdIns4KII enzymes (130, 315).
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MICHAEL G. ROTH
1. PIP5KI␣, PIP5KI␤, PIP5KI␥, and MSS4p
The mammalian PIP5Ks ␣- and ␤-isoforms were
cloned independently from human or mouse by two laboratories and named in a reciprocal manner (157, 209). A
third isoform of PIP5KI, ␥, has also been cloned from both
species (158). Unfortunately, the reciprocal nomenclature
for isoforms ␣ and ␤ has been perpetuated in the genome
sequence databases for human and mouse. This complication of the nomenclature means that one must be careful to note the species of enzyme used in any study. To
simplify the process of specifying which gene product has
a particular function, for the purpose of this review I will
adopt the human genomic nomenclature where PIP5KIA
indicates human PIP5KI␣ and murine PIP5K␤, PIP5KIB is
human PIP5KI␤ and murine PIP5KI␣, and PIP5KIC indicates PIP5KI␥.
PIP5KIA and B are 61-kDa proteins, and C is larger
and has two forms, 87 and 90 kDa, due to alternative
splicing. The kinase domain of PIP5KIs is comprised of
⬃400 amino acids located centrally and is 80% identical
among all three proteins. Phosphatidic acid (PA) has been
shown to stimulate these enzymes (164, 243), and all three
of the PIP5Ks are activated ⬃10-fold by this lipid (158). A
major source of PA is through the hydrolysis of phosphatidylcholine by phospholipases D1 and D2, enzymes that are
themselves activated by PtdIns(4,5)P2 (326). In vitro the
PIP5KIs can phosphorylate phosphoinositides other
than PtdIns(4)P and will convert PtdIns(3,4)P2 to
PtdIns(3,4,5)P3 and PtdIns(3)P to both PtdIns(3,5)P2 and
PtdIns(3,4,5)P3 (106, 356, 409).
The regulation of PIP5KIs is complicated. These enzymes can be precipitated in complexes that contain the
small G proteins Rho and Rac (46, 289, 355), although it is
not known if this is a direct interaction or involves additional proteins. PtdIns(4,5)P2 is an important regulator of
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the actin cytoskeleton, and overexpression of PIP5KIB
causes massive actin polymerization that is not prevented
by coexpression of a dominant negative form of RhoA,
suggesting that the lipid kinase is downstream of Rho
(316). Recently an activator of PIP5KIB was purified and
found to be the small G protein Arf1 (151). Arf1 has many
activities that are important for membrane traffic (293).
Purified Arf1, Arf5, and Arf6, but not RhoA or Rac1, could
stimulate purified PIP5KIB in vitro, and this stimulation
required PA. However, only Arf6 colocalized with
PIP5KIB at the plasma membrane in vivo and is likely to
be the regulator of PIP5KIB relevant to regulation of the
actin cytoskeleton (27, 39, 151). Although an activated
Rac1 allele stimulated membrane ruffles and colocalized
with Arf6 and PIP5KIA, membrane ruffles were prevented
when a dominant negative form of Arf6 was expressed
(151). Thus current data suggest that Arf6 may be downstream of RhoA and Rac1 and interact directly with
PIP5KIB at the plasma membrane.
In addition to regulation by small G proteins,
PIP5KIB is regulated by phosphorylation (266). PIP5K
isolated from Saccharomyces pombe membranes is also
regulated by phosphorylation by Cki1, a casein kinase I
ortholog (362). All three mammalian PIP5Ks will autophosphorylate in vitro, and this is stimulated by PtdIns
but not other phosphoinositides (160). In all cases
documented so far, phosphorylation suppressed PIP5K
activity.
PtdIns(4,5)P2 is important for many aspects of membrane traffic including endocytosis, synaptic vesicle fusion and recycling, regulated exocytosis, phagocytosis,
and vesicle formation at the Golgi (53, 66, 119, 171, 217).
In most cases, systematic comparisons of the PIP5K and
PIP4K isoforms that might be responsible for producing
PtdIns(4,5)P2 for these activities have not been performed. Overexpression of wild-type PIP5KI〈, but not
PIP5KI〉, stimulates internalization of the EGF receptor,
and overexpression of a kinase dead mutant blocks EGFR
endocytosis (14). However, overexpression of PIP5KI〉
and to a lesser extent PIP5KI〈 enhances endocytosis of
the transferrin receptor in a different cell type (262).
Knock-down of PIP5KIB by siRNA, but not knock down of
PIP5KIA or PIP5KIC, inhibits endocytosis of transferrin.
Interestingly, expression of the C isoform was increased
when transcription of either A or B was inhibited, but this
did not result in rescue of endocytosis rates or a change
in total cellular PtdIns(4,5)P2 levels, suggesting that activity of the enzyme is regulated at a posttranscriptional
level (262). PIP5KI〉 can be recruited on to Golgi membranes where it is directly activated by Arf1 (168).
PIP5KIC is the major PIP5K in synapses and is an
important regulator of the recycling of synaptic vesicles
(78, 382).
MSS4 encodes the PIP5K of S. cerevisiae (76, 150)
and is an essential gene (388). Acute loss of MSS4p func-
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phosphorylate PtdIns to PtdIns(5)P in vitro (357) and
could properly be called PI5Ks. However, it is not clear if
they produce PtdIns(5)P in vivo. Due to this uncertainty
and because the type I enzymes are most often referred to
as PIP5Ks in the literature, that term will be used in this
review. Three human PIP5K enzymes have been identified, and all are related to the MSS4p kinase of S. cerevisiae. As major producers of PtdIns(4,5)P2, the PIP5Ks
play important roles in membrane traffic; however, the
precise roles played by the various isoforms of these
enzymes are not yet clear. S. cerevisiae has a second PI
5-kinase, FAB1, that has recently been shown to phosphorylate PtdIns(3)P to produce PtdIns(3,5)P2 (57, 115).
The mouse ortholog of this enzyme has been cloned and
named PIKfyve (306, 320). PtdIns(3,5)P2 is necessary for
proper membrane traffic to the yeast vacuole; thus PIKfyve is very likely to play a similar role in mammalian
cells.
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
tion causes alterations in the actin cytoskeleton but not in
secretion. Currently there are no data supporting a role
for PtdIns(4,5)P2 for secretion in S. cerevisiae, in contrast
to a requirement for PtdIns(4)P (129, 370). There is indirect evidence for a role for PtdIns(4,5)P2 in the internalization step in endocytosis in yeast (154), and by extension, a role for Mss4p in that process.
2. Fab1 and PIKfyve
D. PIP 4-Kinases
Three 48-kDa kinases have been identified that
phophorylate phosphatidylinositol 5-phosphate. PIP4K␣
was originally purified as an activity that phosphorylated
a commercial PtdIns(4)P preparation to PtdIns(4,5)P2 (18,
208) and was named PIP5K type II␣. After this and a
related enzyme, PIP5K type II␤, were cloned (25, 37, 79),
it was discovered that the enzymes actually phosphorylated the D-4 position (283). The actual substrate in the
bovine brain PtdIns(4)P that was used for the original
purification of the enzymes was a previously unidentified
lipid, PtdIns(5)P. Thus these enzymes should be called
PIP4Ks. PIP4K␣ can phosphorylate PtdIns(3)P and
PtdIns(5)P but does not make PtdIns(3,4,5)P3 (283, 409)
and will not phosphorylate PtdIns (106). The PIP4Ks are
also not stimulated by PA (164). Currently little is known
about the roles of these enzymes in cells or if they impact
membrane traffic in any way. PIP4K␤ partially localizes to
the nucleus (49). A third member of this family, PIP4K␥,
has been identified as resident in the ER (159).
Physiol Rev • VOL
E. Phosphatases Acting on Phosphoinositides
As one would expect, cells not only generate PIPs
through phosphorylation but also consume or interconvert them through the action of phosphatases. Many different enzymes have been identified that specifically remove phosphate from one or more of the positions on the
inositol ring (155, 213, 240). There is currently evidence
for a role in membrane traffic for enzymes that remove
phosphate from the D-5 position of PtdIns(4,5)P2, the D-5
position of PtdIns(3,5)P2, the D-3 position of PtdIns(3,5)P
and that remove the phosphate from both PtdIns(4)P and
PtdIns(3)P (Table 2). It is likely that enzymes that specifically hydrolyze phosphate from PtdIns(3,4,5)P3 or
PtdIns(3,4)P2 play roles in signal transduction, but not
directly in membrane traffic. There is currently not much
information about enzymes that remove phosphate only
from the D-4 position of PtdIns(4)P, and S. cerevisiae
does not have homologs to the currently identified mammalian enzymes. It is likely that the important function of
degrading PtdIns(4)P in S. cerevisiae is performed by
Sac1p.
1. Sac family phosphatases
The first lipid phosphatases shown to have a role in
membrane traffic contain a domain originally recognized
in the yeast protein Sac1p. One group of these enzymes
contains only a NH2-terminal Sac domain, and the second
class contains an additional, 5-phosphatase domain in the
center of the protein followed by various other domains
(155). Sac1p was identified in a screen for mutations that
relieved the block in secretion caused by loss of activity
of the S. cerevisiae PITP, Sec14p (51, 385), and was
subsequently discovered to have PIP phosphatase activity
(47, 124). In S. cerevisiae there are two such proteins,
Sac1p and Fig4p, and in humans three, KIAA0274,
KIAA0966, and KIAA0851. Sac1p localizes to the ER and
Golgi (311, 385), and sac1⌬ cells contain 10-, 2.5-, and
2-fold increases in PtdIns(4)P, PtdIns(3,5)P2, and
PtdIns(3)P, respectively (124). In the ER, Sac1p is necessary for ATP import into the lumen (224), but it also has
important phosphatase function antagonizing the PtdIns
4-kinase Pik1p in the Golgi. Fig4p is induced by pheromone and required for actin polarization during mating
(96). KIAA0274 is probably the human ortholog to yeast
Sac1p, and KIAA0851 is probably the Fig4p ortholog.
KIAA0966 is a large protein of unknown function. The
catalytic Sac domains of all these proteins except
KIAA0966 hydrolyze PtdIns(3)P, PtdIns(4)P, and
PtdIns(3,5)P2, but not PtdIns(4,5)P2 (155). KIAA0966 is a
5-phosphatase with preference for PtdIns(4,5)P2 over
PtdIns(3,4,5)P3 (236).
The second group of Sac domain phosphatases includes the yeast proteins Ins51p (Slj1p), Inp52p (Slj2p),
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Fab1p is the PI3P 5-kinase in S. cerevisiae and is
required for maintenance of the vacuole, although not for
membrane traffic to the vacuole (57, 115, 399). A mouse
homolog of FAB1 has been cloned (306). Sequence homology searches reveal that the human Fab1 ortholog
PIKfyve is encoded by a single gene on chromosome 2.
Both PIKfyve and Fab1p contain a domain called a FYVE
domain (see below) that binds to PtdIns(3)P, and in the
case of PIKfyve, is required for the enzyme to locate on
endosomes (308). PIKfyve will phosphorylate PtdIns or
PtdIns(3)P to PtdIns(5)P or PtdIns(3,5)P2, respectively,
and also has intrinsic protein kinase activity (307). Like
the PI5Ks, PIKfyve phosphorylates itself, and this inhibits
its lipid kinase activity (307). Overexpression of a mutant
PIKfyve able to produce PtdIns(5)P but unable to produce
PtdIns(3,5)P2 causes extensive vacuolation of cells that is
rescued by microinjecting them with PtdIns(3,5)P2 but
not PtdIns(5)P (156). Thus PtdIns(3,5)P2 appears to be a
product of PIKfyve in vivo required for endosome function.
705
706
MICHAEL G. ROTH
TABLE
2.
PIP phosphatases that function in membrane traffic
Enzyme
Cellular Location or
Ortholog
5-Phosphatases
OCRL
Synaptojanin 1
Golgi
Clathrin coats
(nerve terminals)
Synaptojanin 2
Clathrin coats
(ubiquitous)
Inp51p (Slj1p)
?
Inp52p (Slj2p)
?
Inp53p (Slj3p)
TGN
In54p
ER
Sac domain phosphatases
KIAA0274
Sac1 ortholog
Molecular
Weight
Substrate
Product
Reference Nos.
Mammalian
Mammalian
75
145
PtdIns(4,5)P2
PtdIns(4,5)P2
PtdIns(4)P
PtdIns
87, 344, 360, 407, 408
124, 127, 227
Mammalian
138
PtdIns(4,5)P2
PtdIns
124, 254
S.
S.
S.
S.
108
118
124
48
PtdIns(4,5)P2
PtdIns(4,5)P2
PtdIns(4,5)P2
PtdIns(4,5)P2
PtdIns(4)P
PtdIns
PtdIns
PtdIns(4)P
19, 124–126, 260, 338
Mammalian
100
PtdIns(3)P,
PtdIns(4)P,
PtdIns(3,5)P2
PtdIns(4,5)P2
PtdIns(3)P,
PtdIns(4)P,
PtdIns(3,5)P2
PtdIns(3)P,
PtdIns(4)P,
PtdIns(3,5)P2
PtdIns(3)P,
PtdIns(4)P,
PtdIns(3,5)P2
PtdIns
155, 236
Species
cerevisiae
cerevisiae
cerevisiae
cerevisiae
?
Fig4 ortholog
Mammalian
Mammalian
100
65
Sac1p
ER, Golgi
S. cerevisiae
71
Fig4p
Vacuole?
S. cerevisiae
102
?
?
Mammalian
Mammalian
66
71
MTMR3
?
Mammalian
128
MTMR6
?
Mammalian
68
Ymr1p
(YJR110w)
?
S. cerevisiae
80
3-Phosphatases
MTM1
MTMR2
PtdIns
PtdIns
PtdIns
47, 51, 124, 385
PtdIns
96, 114
PtdIns(3)P
PtdIns(3)P,
PtdIns(3,5)P2
PtdIns(3)P
PtdIns(3,5)P2
PtdIns(3)P
PtdIns(3,5)P2
PtdIns
PtdIns
309, 350
PtdIns(3)P
PtdIns
PtdIns
PtdIns
350
TGN, trans-Golgi network. Other definitions are as in Table 1.
and Inp53p (Slj3p) and mammalian proteins synaptojanin
1 and 2. The phenotypes of cells with null mutations in
either INP51, INP52, or INP53 are relatively normal, but
deletion of all three is lethal (332, 343). Ins51p is a 5-phosphatase specific for PtdIns(4,5)P2, and its Sac domain is
inactive (124). INS51 has genetic interactions with PAN1,
a protein required for endocytosis and regulation of actin
(380). Inp52p and Inp53p have both 5-phosphatase activity as well as Sac domain phosphatase activity and are
involved in regulating actin patches at the plasma membrane (PM) (260, 338). Disruption of INP53, but not INP51
or INP52, causes sorting defects at the TGN and increases
the rate of transport of reporter proteins to the vacuole
(19, 125). This is due to a defect in the pathway between
the TGN and early endosomes that requires AP1/clathrin
(126). This defect is more severe in an inp52⌬ inp53⌬
mutant and is complemented by a mutant inp52 lacking
Sac phosphatase activity, indicating that it is the excess
PtdIns(4,5)P2 that is the primary problem in these cells
(338). Double mutants inp51⌬ inp52⌬ or inp52⌬ inp53⌬,
but not inp51⌬ inp53⌬, have defects in endocytosis and
disruption of the actin cytoskeleton (327, 332, 343). This
Physiol Rev • VOL
suggests that Inp52p has overlapping function with the
other two enzymes. In inp51⌬ inp53⌬ inp52ts cells at
nonpermissive temperature, PtdIns(4,5)P2 is detected on
internal membranes where it is normally not detected
(338). Thus these enzymes control the location of
PtdIns(4,5)P2 in S. cerevisiae.
Synaptojanin 1 and 2 are dual-function mammalian
phosphatases that contain a 5-phosphatase activity as
well as a Sac domain and convert PtdIns(4,5)P2 to PtdIns
(124). This ability to decrease PtdIns(4,5)P2 without producing the potentially active intermediate PtdIns(4)P may
be important for maintaining spatial segregation of PIPs
(discussed below). Synaptojanin 1 is found in nerve terminals associated with membranes coated with clathrin
(127, 227). Mice deficient in synaptojanin 1 (67, 181) and
mutants in Unc26, the C. elegans synaptojanin ortholog
(134), have neurological defects and nerve endings that
accumulate coated vesicles, suggesting that there is a
defect in vesicle uncoating. Synaptojanin 2 has a broader
tissue distribution and differs from synaptojanin 1 at the
COOH terminus (254). Synaptojanin 2 is reported to be an
effector for the small GTPase Rac1, and overexpression
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KIAA0966
KIAA0851
389
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
of activated Rac1 or a synaptojanin 2 targeted to membranes inhibits endocytosis (214). Depletion of synaptojanin 2, but not synaptojanin 1, by small interfering RNA
decreased internalization of epidermal growth factor
(EGF) and reduced numbers of coated pits in lung carcinoma cells (299).
2. Other 5-phosphatases
3. 3-Phosphatases
PTEN/MMAC1, myotubularin, and myotubularin-related proteins are phosphatases specific for the D-3 position of phosphoinositols (212). PTEN hydrolyzes
PtdIns(3,4,5)P3 and is a negative regulator of signaling. It
probably has no direct role in membrane traffic. Myotubularin (MTM1) was identified as the defective gene in
X-linked myotubular myopathy, a defect in muscle development. Mutations in a related gene, MTMR2, cause type
4B Charcot-Marie-Tooth syndrome. There are eight myotubularin-related genes in humans and one in S. cerevisiae (YMR1). Recombinant MTM1, MTMR2, MTMR3
(KIAA0371), MTMR6, and Ymr1p proteins are active
PtdIns(3)P
phosphatases
that
also
hydrolyze
PtdIns(3,5)P2 (309, 350). The activity of MTM1 toward
PtdIns(5)P in vitro is 200-fold less than for PtdIns(3)P,
and other phosphoinositides are significantly poorer substrates (350). The physiological function of MTM family
members is not known. However, MTMR3 contains a
COOH-terminal FYVE domain for binding to PtdIns(3)P,
as do a number of proteins that bind to endosomes, and
may be a candidate for an enzyme responsible for controlling the amount and/or location of that lipid on endosomal membranes.
III. PHOSPHOINOSITIDE-BINDING MODULES
THAT FUNCTION IN CONSTITUTIVE
MEMBRANE TRAFFIC
The second discovery suggesting that phosphoinositides might be important for regulating constitutive
Physiol Rev • VOL
membrane traffic was the realization that some proteins
known to be required for membrane traffic contained a
motif, the pleckstrin homology (PH) domain, known to
bind PtdIns(4,5)P2. Subsequently, three additional motifs,
the FYVE, ENTH, and PX domains, were identified in
many proteins including some that had been identified
through screens for mutations that affected membrane
traffic in S. cerevisiae. These modules were subsequently
shown to bind phosphoinositides. In certain proteins,
these lipid-binding domains show great specificity for one
phosphoinositide, but in most cases, they will bind to
more than one species. A current unresolved problem is
that in vitro many of these modules will show higher
affinity for PtdIns(3,4,5)P3 than other PIPs. However, it is
unclear if this difference in affinity is enough to be meaningful in the cell, where PtdIns(3)P, PtdIns(4)P, and
PtdIns(4,5)P2 are 50 –1,000 times more abundant than is
PtdIns(3,4,5)P3.
A. PH Domains
The PH domain was first identified as a sequence
motif of 100 –120 amino acids that was found in many
signaling proteins as well as in the cytoskeletal protein
spectrin (135, 223, 246). In phosphoinositide-specific
phospholipase C-␦1 (246), the PH domain was located in
the region previously shown to bind to PtdIns(4,5)P2 (48).
Subsequently the PH domains from several proteins were
found to bind specifically to liposomes containing
PtdIns(4,5)P2 (133). Primary sequence conservation
among different PH domains is only 7–30%, but the structures that have been solved are quite similar. PH domains
have a seven-stranded, antiparallel ␤-sheet that is twisted
to fold back on itself as an orthogonal sandwich (100, 204,
288, 303). Most PH domains have strong charge polarity
with one edge of the curved sheet much more positive
than the other. The positive side interacts with the negative head group of the lipid. The affinity and specificity
with which different PH domains bind phosphoinositides
vary greatly. Most have only weak affinity (KD of 30 – 40
␮M) (133, 303), but some bind 10 –1,000 times more
tightly, especially those specific for PtdIns(3,4,5)P3 (200).
The concentration of PtdIns(4,5)P2 in neutrophil plasma
membranes has been estimated as 3–5 mM and that of
PtdIns(3,4,5)P3 at 5 ␮M (basal) to 200 ␮M (after stimulation) (341). Thus, unless a PH domain exhibits 25- to
1,000-fold greater affinity for the PtdIns(3,4,5)P3 than
PtdIns(4,5)P2, it is unlikely to bind selectively in the cell.
A KD in the range of 30 ␮M means that stable binding to
membranes by low-affinity PH domains should require
additional interactions and experimental evidence supports this. In many if not most cases, stable membrane
binding of proteins that contain PH domains involves
interaction with other segments of the same protein, or
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Inp54p, the fourth 5-phosphatase enzyme in S. cerevisiae, lacks a sac domain and has a single 5-phosphatase domain. It localizes to the ER, and its deletion increases the rate of secretion of a reporter, indicating that
it functions directly or indirectly in secretion (389). In
mammals there are a number of other 5-phosphatases,
most of which have been investigated for roles in signal
transduction or apoptosis, but not membrane traffic.
However, the OCRL gene product that is defective in the
human disease Lowe syndrome is a 5-phosphatase that
localizes to the TGN (87, 344, 408). Kidney cells from
patients with Lowe syndrome have elevated PtdIns(4,5)P2
levels (407) as well as elevated serum levels of lysosomal
enzymes (360), raising the possibility that there is a defect
in sorting proteins at the TGN.
707
708
MICHAEL G. ROTH
B. PX Domains
PX, or phox (phagocyte oxidase), homology domains
are found in two subunits of NADPH-oxidase, in PI3KC2␥
and in a family of small proteins called sorting nexins
(SNX) (128, 277). They are also found in certain other
yeast proteins known to be required for protein traffic
between the Golgi and endosomes (91, 153, 368) and in
TABLE
3.
Proteins containing PH domains known or suspected to function in membrane traffic
Proteins
Lipid Bound
Function of Protein
Function of Domain
Reference Nos.
Required for budding
of clathrin-coated
vesicles
Known and potential
Arf GEFs
Modulates dynamin
GTPase activity and
protein binding
Stimulates activity and
contributes to
membrane location
2, 16, 142, 171,
184, 196,
361, 402
163, 177, 183
PtdIns(3,4,5)P3,
PtdIns(4,5)P2
Arf GAPs
Determines membrane
location and
stimulates GAP
activity
30, 162, 163,
174, 285
PtdIns(4,5)P3
Convert PC to PA
145, 345
?
PtdIns(4,5)P2
Converts DAG to PA
Kinesin family motors
Determines membrane
location and
stimulates activity
?
Binds to cargo vesicles
Dynamins 1,2,3
PtdIns(4,5)P2
B2-1/cytoshesin-1/Sec7A/PSCD1
Cytohesin-2/ARNO1/Sec7B/PSCD2
GRP1/cytohesin-3/ARNO3/Sec7C
Cytohesin-4/dj63g5.1
EFA6/PSD/cytohesin5
Tdic/cytohesin-6
HCAA67/cytohesin-7
ASAPs
ASAP1/centaurin ␤4/DEF1
ACAP1/centaurin ␤1
ACAP2/centaurin ␤2
PAP␣,␤/PAG3/centaurin ␤3
Centaurin ␦1/ARAP2
Centaurin ␦2/ARAP1
PLD1
PLD2
PtdIns(3,4,5)P3
DGK␦
KIF1A
KIF1B
phospholipase D1 (PLD1) and phospholipase D2 (PLD2)
(105) (Table 4). The SNX proteins were key to understanding the function of the PX domain. The first sorting
nexin family member, SNX1, had been identified as a
protein that bound to the EGF receptor and that had
sequence homology to a yeast protein known to function
in membrane traffic to the vacuole (192). Subsequently, a
number of SNX proteins have been shown to associate
with specific membrane receptor proteins as part of an
oligomeric complex that regulates sorting of receptors
between recycling and degradation pathways (128, 153,
342). SNX proteins appear to associate into complexes
with other SNX proteins, as well as with adaptor proteins
that bind to receptors and to clathrin (193, 206, 211, 267).
The fraction of the genome devoted to SNX proteins in S.
cerevisiae is threefold greater than it is in the human
genome. Therefore, most SNX proteins probably function
in evolutionarily conserved processes common to most
cell types. Evidence for the functions of SNX proteins
currently is dominated by results of experiments in which
wild-type or mutant forms are overexpressed as dominant
negative inhibitors of endocytosis. Because overexpression of one member of a family of proteins can affect
processes unrelated to the normal function of that protein, more work is needed to determine where each human SNX protein functions.
There are 31 human genes predicted to encode proteins with PX domains and 15 in S. cerevisiae. PX
domains from different proteins have been shown to
PtdIns(3,4,5)P3
PtdIns(4,5)P2(?)
249
185
DAG, diacylglycerol; PC, phosphatidylcholine; PA, phosphatidic acid; GEFs, guanine nucleotide exchange factors; GAPs, GTPase accelerating
proteins.
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interaction with additional proteins (184, 196 –198). Binding to phosphoinositides has not been observed to alter
the conformation of the PH domain (133), although it may
change the interaction between the PH domain and another domain in the same protein (23).
Of the 251 PH domains identified in the human proteome, 20 or so have a conserved motif that allows highaffinity binding to PtdIns(3,4,5)P3 or PtdIns(3,4)P2 (100,
204) and probably function in signal transduction (200).
Many of the remaining proteins do not yet have known
functions, and some of these may contribute to membrane traffic. The proteins known to function in membrane traffic that contain PH domains include the three
dynamin GTPases, some of the guanine nucleotide exchange proteins for Arf family members, some of the
GTPase activating proteins for Arf, two kinesin motor
proteins, and several lipid modifying enzymes (Table 3).
Additional information on PH domains and the proteins
that contain them can be obtained from recent review
articles (23, 200, 278, 303).
709
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
TABLE
4.
PX domain proteins known to function in membrane traffic
Proteins
Function of Protein
PtdIns(3)P
Transport from Golgi to vacuole
Golgi to endosome traffic
SNX3 homolog, retains proteins in TGN
Retrograde transport from endosomes to Golgi
Retrograde transport from endosomes to Golgi
40, 304, 328
91
368
153, 257
153
PtdIns(3)P
Sorting receptors (EGFR) for downregulation
Associates with growth factor receptors
Retrograde transport from endosomes to Golgi
Sorting receptors (EGFR) for downregulation
Associates with TGF-␤ receptors
EGF receptor downregulation
Endosomal protein traffic
Endocytosis of LDL receptor family proteins
Membrane localization
Membrane localization
65, 128, 192, 411
128
128, 397
128
267
206, 211
15, 272
342
97, 278, 345
97, 278, 345
PtdIns(3)P
Reference Nos.
TGF, transforming growth factor; EGF, epidermal growth factor; LDL, low-density lipoprotein.
bind preferentially to PtdIns(3)P, PtdIns(3,4)P2, or
PtdIns(4,5)P2 (40, 94, 175, 328, 397, 398). However,
PtdIns(3)P is much more abundant than other D-3 phosphoinositides and may represent the major lipid bound in
the cell by PX domains that prefer a D-3 phosphate. Many
PX domains also contain a binding motif for SH3 domains
(143) or are found adjacent to coiled coil domains (351,
411). As is the case for PH domains, the membrane location of proteins containing PX domains is probably specified by protein-protein interactions as well as by lipid
binding. Additional information on proteins containing PX
domains can be obtained from recent reviews on this
subject (93, 305, 393, 398).
C. FYVE Domains
The FYVE domain, named as a acronym for the first
four proteins in which it was recognized (340), is a type of
zinc finger that binds to PtdIns(3)P (32, 117, 269). The
signature of this domain is a defined spacing of cysteines
that coordinate zinc and three additional blocks of residues that participate in lipid binding. Stenmark et al. (339)
have identified 27 FYVE domain proteins in humans, 15 in
C. elegans, and 5 in S. cerevisiae (339). Automated sequence analysis tools report larger numbers of FYVE
domains in these organisms. EEA1, one of the four proteins in which the FYVE domain was first recognized,
binds to early endosomes. The FYVE domain of EEA1 is
necessary, but not sufficient, for this binding (35, 194).
The COOH-terminal portion of EEA1 contains a coiledcoil domain and terminates in the FYVE domain. The
crystal structure of this COOH-terminal fragment reveals
a dimer held together through interactions between the
two coiled coil domains and between one edge of each of
the two FYVE domains. Together, the FYVE domains form
Physiol Rev • VOL
a flat surface orthogonal to the coiled coil domain. Residues that contact the lipid head group are on the face of
the protein opposite the coiled coil, and four hydrophobic
residues near the phosphate binding residues form a loop
that would dip down into the hydrophobic core of the
bilayer (88). Thus, in EEA1, specificity of the head groupbinding pocket is supplemented by nonspecific hydrophobic interactions as well as strengthened by being bivalent.
A similar mode of binding has been reported for the FYVE
domains of Vps27p and Hrs (335), and it is likely that
FYVE domains, like PH and PX domains, use multiple
contacts to achieve proper membrane location.
Proteins containing FYVE domains have been shown
to function in endocytosis, in growth factor signaling, and
in regulation of the actin cytoskeleton (62, 339, 396) (Table 5). Proteins with the first two functions are found on
endosomes, and those of the last class, which also contain
multiple PH domains, are found on the plasma membrane.
The arrays of other domains found in proteins that contain FYVE domains suggest that many of them will assemble into multiprotein complexes. Table 5 lists proteins
known or thought to function in membrane traffic that
contain FYVE domains.
D. ENTH/ANTH Domains
The ENTH (epsin 1 NH2-terminal homology) domain
was originally recognized as an NH2-terminal sequence in
epsin 1 and several other proteins that had known or
suspected roles in endocytosis (41, 178). This region of
one of these proteins, AP180, had previously been shown
to bind to inositol hexakisphosphate (403), and the ENTH
domain was found to be a phosphatidylinositol binding
module preferring PtdIns(4,5)P2 (104, 161). However,
structural data showed that proteins related to AP180 and
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S. cerevisiae
Vam7p
Mvp1p
Grd19p
Vps5p
Vps17p
Mammalian
SNX1
SNX2
SNX3
SNX4
SNX6
SNX9
SNX15
SNX17
PLD1
PLD2
Lipid Bound
710
MICHAEL G. ROTH
TABLE
5.
Proteins that contain FYVE domains and function in membrane traffic
Protein
Lipid Bound
Function of Protein
S. cerevisiae
Vac1p
PtdIns(3)P
Vps27p
Fab1p
PtdIns(3)P
PtdIns(3)P
Rabenosyn-5 ortholog
Adaptor protein binding Rab5 and effectors
Hrs ortholog, required for sorting into multivesicular bodies
PtdIns(3)P 5-kinase required for formation of multivesicular
bodies, PIKfyve ortholog
Mammalian
EEA1
PtdIns(3)P
PtdIns(3)P
PIKfyve
PtdIns(3)P
Rabenosyn-5
Rabip4/RUFY1
FERG-1/DFCP1
MTMR3
PtdIns(3)P
CALM have a NH2-terminal domain with a distinct fold
(ANTH domain). The ANTH domain binds the phosphoinositide head group via solvent-exposed basic residues
(104), whereas the ENTH domain binds the lipid in a
pocket that contacts the head group as well as the attached glycerol (103). Binding of PtdIns(4,5)P2 by the
ENTH domain causes the NH2-terminal helix of the domain to penetrate into the lipid bilayer, slowing membrane dissociation of the domain and inducing membrane
curvature (103, 336). Proteins that contain ENTH/ANTH
domains also contain multiple recognition motifs for
other types of protein-protein interaction modules and
probably function as scaffold proteins that assemble protein complexes on membranes (73).
The ANTH domain proteins AP180 and CALM bind to
clathrin and AP2 adaptors and are proposed to nucleate the
polymerization of the clathrin coat (172). Epsin1 binds to the
AP2 ␣- and ␤-ear domains, and another family member,
EpsinR, binds to the AP1 ␥-ear domain and to GGA1–3 at the
TGN (144, 173, 235, 373). EpsinR contains an acidic phenylalanine motif found in two yeast proteins, Ent3p and Ent5p,
that is necessary for them to bind to AP1 and Gga2p (89, 90,
235). EpsinR shows preference for binding to PtdIns(4)P
and PtdIns(5)P in vitro (144, 235), which is consistent with
the finding that PtdIns(4)P is abundant on Golgi membranes
(372). Epsin and EpsinR contain a ubiquitin binding domain
just COOH terminal to the ENTH domain and are themselves monoubiquitylated (146, 182, 259, 276). Ubiquitylation
of hormone receptors (202, 210), as well as certain other
membrane proteins (108), is necessary for sorting them in
early endosomes from the recycling to the degradative pathway. It is less clear what role ubiquitylation would have for
a protein that functions in TGN to endosome sorting, such as
Physiol Rev • VOL
33, 255, 271, 348, 378
22, 188, 274
57, 115, 399
34, 116, 194, 195, 270, 325, 340
45, 188, 280, 317, 347
156, 306, 308
255
61, 216, 400
290
371
EpsinR (144, 235). In yeast, monoubiquitylation also serves
as a signal for internalization from the plasma membrane
(353). Internalization of the mammalian growth hormone
receptor apparently requires that it be recognized by ubiquitylation machinery, but the actual ligation with ubiquitin is
not necessary for internalization (300). The proteins that
recognize ubiquitylated receptors on endosomal membranes, such as Hrs, are themselves monoubiquitylated (276,
280, 317). Although detailed knowledge of the precise interactions is lacking, it appears that the ENTH domain of the
epsins links a membrane recognition event regulated by
PtdIns(4,5)P2 and perhaps PtdIns(4)P to another membrane
recognition event regulated by PtdIns(3)P through the FYVE
domain of Hrs.
Two other proteins that contain ENTH domains,
HIP1 and HIP1R, and their counterpart in S. cerevisiae,
Sla2p, interact with the actin cytoskeleton as well as play
a role in endocytosis (95, 232, 238, 369, 383, 401). Phosphatidylinositides play a major role in regulating actin
(404), and the ENTH domains of HIP1 and HIP1R may
function to coordinate the assembly of endocytic coat
proteins with changes in the actin cytoskeleton. A list of
human proteins containing ENTH domains and thought to
function in membrane traffic is presented with their yeast
orthologs in Table 6.
E. Basic Sequences and Other Motifs That
Bind Phosphoinositides
In addition to the modular phosphoinositide binding
motifs, a number of binding sites have been identified that
have in common clusters of basic residues interspersed
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Hrs
Rab 5 effector on early endosomes regulating endosomes
fusion
Required for receptor sorting in endosomes to the
degradative pathway
Binds ubiquitinylated receptors to clathrin-coated
endosome membranes
PtdIns 5-kinase producing PtdIns(3,5)P2 required for
endocytic organelle structure
Rab5 effector linking Rab 5 to hVPS45
Required for correct sorting of cathepsin D
Rab4 effector required for recycling from endosomes, binds
etk tyrosine kinase
Overexpression disturbs Golgi structure
PtdIns(3)P and PtdIns(3,5)P2 phosphatase
Reference Nos.
711
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
TABLE
6.
Proteins containing ENTH/ANTH domains thought to function in membrane traffic
Protein
S. cerevisiae
Ent1
Lipid Bound
Function of Protein
Nonspecific binding
of PIPs
Epsin ortholog; binds clathrin and actin-binding protein Pan1 and is
required for endocytosis
Epsin ortholog, binds clathrin and is required for endocytosis
Binds Gga2 and AP1␥ and colocalizes with clathrin on Golgi; ent3⌬
ent5⌬ cells have defects in carboxypeptidase S transport
Same as Ent3
Ortholog of HIP1 and HIP1R/HIP12; binds actin and loss causes
defects in actin and endocytosis
Ent2
Ent3
Ent5
Sla2p
Mammalian
Epsin 1
PtdIns(4,5)P2
Epsin 2
CLINT
PtdIns(4,5)P2
PtdIns(4)P,
PtdIns(3,5)P2,
PtdIns(4,5)P2,
PtdIns(3,4,5)P3
3, 381
381
89, 90
89, 90
95, 383, 401
41, 104, 242
292
330
373
232, 238, 369
95
104, 131, 207, 256, 403
352
173
Man 6-P, mannose 6-phosphate.
with hydrophobic residues and little other primary sequence conservation. These have been found in many
cytoskeletal proteins (reviewed in Refs. 218, 404), clathrin
adaptor proteins (55, 111, 132), C2 domains (38, 60),
including in synaptotagmin (310) and in PLD (314, 410).
PLD1 and PLD2 contain both PX and PH domains, but the
site that binds PtdIns(4,5)P2 that regulates enzyme activity is a conserved sequence of the basic/hydrophobic type
found in PLD1, PLD2, yeast Spo14, and less conserved in
plant PLDs. The lesson from this example is that the
observation that a protein is regulated by a phosphoinositide and contains a known phosphoinositide-binding
module does not necessarily lead to the conclusion that
the module regulates protein activity. The number of
examples of proteins with multiple phosphoinositide
binding sites is increasing rapidly.
PHD domains are orphan zinc-finger domains found
in a large number of nuclear proteins (1). ING2, a protein
that associates with histone acetyltransferase and histone
deacetylase complexes (99), was identified as a protein
that bound to a phosphoinositide resin (121). ING2 bound
preferentially to PtdIns(5)P and PtdIns(3)P through its
PHD domain, as did several other proteins with PHD
domains. The PHD domain is structurally similar to a
FYVE domain (239, 268), and basic residues in the ING2
PHD domain predicted to be on a surface analogous to the
PtdIns(3)P binding surface of the FYVE domain were
found to be necessary for binding PtdIns(5)P (121). No
Physiol Rev • VOL
protein known to be important for membrane traffic has
been identified that has a PHD domain.
IV. INTRACELLULAR DISTRIBUTION AND
FUNCTION OF PHOSPHOINOSITIDES
FOR MEMBRANE TRAFFIC
It is likely that the PIPs important for constitutive
membrane traffic are the more abundant ones (see Fig. 1).
An exception to this may be PtdIns(3,5)P2, which has
been shown to be important for function of the vacuole in
yeast, but about which very little quantitative data exist.
Together, PtdIns and the PIPs are ⬍10% of cellular lipids.
Of this total, 5% is PtdIns(4)P (0.5% total lipids) and 5% is
PtdIns(4,5)P2 (282). Because all PIPs are confined to the
inner leaflet, PtdIns(4)P and PtdIns(4,5)P2 would each be
1% of inner leaflet lipids. Depending on the cell type, the
plasma membrane can be from 2 to 10% of total membranes and the Golgi 7–12% (5, 122). Thus, if the major
pool of PtdIns(4,5)P2 is in the plasma membrane and
PtdIns(4)P is on the Golgi (see below), these two lipids
could be 5% or more of the cytoplasmic leaflet of the
organelle where they are concentrated. Because these
lipids are not uniformly distributed in the membranes that
contain them, their local concentration is likely to be
higher. Less than 0.25% of total inositol lipid is phosphorylated on D-3 (this equals 0.05% of inner leaflet lipid)
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Epsin 3
EpsinR/epsin
4/enthoprotin
HIP1
HIP1R/HIP12
AP180
CALM
Binds AP2, receptors, and overexpression inhibits clathrin-mediated
endocytosis
Associates with AP2 and clathrin and overexpression inhibits
clathrin-mediated endocytosis
Induced in migrating keratinocytes
Colocalizes with AP1, binds GGA2, and stimulates clathrin
assembly
Binds clathrin and AP2
Binds to actin and to clathrin-coated vesicles
Binds clathrin and AP2 and facilitates clathrin assembly in vitro
Binds clathrin heavy chain at PM and Golgi; overexpression inhibits
clathrin-mediated endocytosis and distribution of Man 6-P
receptors
Binds AP1, found on Golgi and copurifies with clathrin-coated
vesicles
Reference Nos.
712
MICHAEL G. ROTH
(282). In murine fibroblasts, the ratio of PtdIns(3)P to
PtdIns(3,5)P2 is 4:1 (384), and in unstimulated neutrophils, the ratio of PtdIns(3)P2 to PtdIns(3,4,5)P3 and
PtdIns(3,4)P2 is 8:1 (341). Thus PtdIns(3)P is ⬃0.04% of
total membrane phospholipid. Endosomes and lysosomes
are ⬃2% of cellular membranes, and if most of the
PtdIns(3)P is present in the endosomal pathway, then
PtdIns(3)P in the cytoplasmic leaflet of endosomes is ⬃4%
of phospholipid and as abundant as PtdIns(4,5)P2 at the
plasma membrane or PtdIns(4)P at the Golgi.
The sites in the cell where each of these lipids function have been inferred from the locations of the proteins
that make, consume, or bind to them, or from studies with
inhibitors of their production. A third method for locating
specific PIPs has been to fuse the lipid binding modules
specific for a PI species to green fluorescent protein
(GFP) or one of its spectral variants (11). A caveat of
these experiments is that lipid-binding modules also interact with proteins, so the labeled membrane may be the
place where both the target lipid and protein colocalize.
The affinity of these binding modules for their target lipid
Physiol Rev • VOL
A. PtdIns(4,5)P2 at the Plasma Membrane
Most of the PtdIns(4,5)P2 in the cell is in the plasma
membrane (11, 375). PtdIns(4,5)P2 is enriched in detergent-resistant membranes (152), and PtdIns(4,5)P2 that is
turned over in response to hormone signaling may be
enriched in caveolae or lipid raft membranes (273). However, recent studies by light or electron microscopy suggest that PtdIns(4,5)P2 is not especially concentrated in
caveolae at steady-state (364, 375). Thus the degree of
subcompartmentalization of PtdIns(4,5)P2 in the plasma
membrane is currently uncertain. PtdIns(4,5)P2 is generated during the process of fusion of regulated secretory
vesicles or synaptic vesicles with the plasma membrane
(66, 219), at the locations where actin rearrangements
occur (59, 67, 404), and is required for clathrin-mediated
endocytosis (67, 104, 161, 171, 262). Although required for
vesicle fusion at the plasma membrane and for homotypic
fusion of yeast vacuoles in vitro (222), the role of
PtdIns(4,5)P2 in vesicle fusion is not known precisely. In
the vacuole fusion reaction, PtdIns(4,5)P2 is required at
the priming step where SNARE protein complexes are
dissociated and also after the docking of the vesicle but
prior to fusion (222). During dense-core vesicle secretion
in mammalian cells, PtdIns(4,5)P2 is detected mainly on
the plasma membrane rather than on the vesicles (149,
219). In PC12 cells, the small GTP-binding protein Arf6
regulates the pool of PtdIns(4,5)P2 required for dense-
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FIG. 1. The major phosphoinositide species are concentrated at
distinct sites in intracellular membrane traffic pathways and may serve
as organelle markers. The major concentration of phosphatidylinositol
4-phosphate [PtdIns(4)P] (blue) is at the Golgi complex, and very little
free PtdIns(4)P is detected at the plasma membrane or on endosomes.
PtdIns(3)P (green) is concentrated on early endosomes. The majority of
phosphatidylinositol 4,5-bisphosphate [PtdIns(4,5)P2] (red) is at the
plasma membrane at steady state. PtdIns(3,5)P2 (orange) is found on
multivesicular endosomes and lysosomes. Some phosphoinositides are
found in the endoplasmic reticulum and in the nucleus, but probably do
not play major roles in membrane traffic.
is often low, but reagents with greater avidity have been
developed by constructing recombinant proteins containing multiple binding motifs (118). These fusion proteins
can tell us where free pools of PIPs are located, but when
used at levels that do not compete with cellular processes, they probably do not detect PIPs that are already
bound to proteins (11). At higher expression levels, they
will interfere with the normal regulation of PIP production. With these limitations in mind, PtdIns(3)P has been
detected primarily on endocytic membranes (32, 92, 318),
PtdIns(4,5)P2 at the plasma membrane (148, 149, 219, 234,
365) and on internal membranes enriched in lipid rafts
(27, 297), and PtdIns(4)P on the Golgi (13, 201, 372).
PtdIns4K activity has been detected in cell fractions enriched in lysosomes (7, 54, 56). From the consequences of
inhibiting its production, PtdIns(3,5)P2 has been inferred
to be present in multivesicular endosomes (MVEs), on the
yeast vacuole, and presumably mammalian lysosomes.
Because all of these membranes are connected by membrane traffic, PIPs must be sorted by segregation into lipid
domains and/or their distribution is maintained dynamically through local lipid production and turnover. Experiments in which lipid phosphatases are deleted in mice, C.
elegans, or yeast indicate that turnover of PIPs is required
to maintain their intracellular location (67, 134, 338).
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
Physiol Rev • VOL
eral cell types (262). This shows that the rates of constitutive endocytosis not only require PIPs, but also might be
regulated through the control of PIP5KI activity. In HeLa
cells, PIP5KIB is responsible for most of the cellular
PtdIns(4,5)P2 with a minor contribution by PIP5KIA and
no detectable contribution of PIP5KIC long or short isoforms (262). However, inhibition of PIPK5IA or PIP5KIC
by small interfering RNA increases transcription of both
of the remaining two isoforms, indicating that although
isoforms A and C do not impact total cell PtdIns(4,5)P2
levels very much, their presence is sensed by the cell and
all three lipid kinases are coordinately regulated (262).
PIP5KIA has been shown to bind to the EGF receptor and
accelerate EGF receptor internalization (14). PIP5KIC is
the major producer of PtdIns(4,5)P2 in the synapse and
probably responsible for the PtdIns(4,5)P2 required for
endocytosis of synaptic vesicle components (382). Thus
different PIP5KI enzymes may potentially regulate endocytic rates of different types of cargo.
There is a correlation in both time and space between
the formation of endocytic vesicles and the reorganization of the actin cytoskeleton (107, 214, 327, 380, 382). In
S. cerevisiae, where clathrin is not required for endocytosis, actin plays a crucial role (245). In mammalian cells,
clathrin, AP2, and dynamin bind to proteins that also bind
to actin (154, 180, 199, 229, 244, 279, 390). The functional
consequence of these two events is not understood at
present. It is possible that cortical actin is a barrier to the
budding of a clathrin coat and must be reorganized so that
a coated vesicle can move away from the cell surface.
However, rather than depolymerize, actin polymerizes as
coated vesicles move away from the membrane (229). In
an early study of the distribution of clathrin coats on
membranes of primary human fibroblasts, Anderson et al.
(6) observed that clathrin-coated pits that contained lowdensity lipoprotein (LDL) receptors lined up over stress
fibers. A more recent study by light microscopy of GFPclathrin in live cells confirms that clathrin coats appear to
organize in relation to cortical actin (302). However, a
caveat to these experiments is that clathrin forms two
structures on plasma membranes, flat lattices and curved
pits. It has been assumed that flat clathrin is the precursor
to curved clathrin pits, but this has never been proven.
Recently, clathrin has been shown to interact dynamically, binding and releasing from the clathrin lattice (394).
Thus the binding and release of GFP-clathrin from membranes cannot necessarily be equated with the formation
and fission of clathrin-coated pits.
Overexpression of PIP5KIB causes actin tails to form
on vesicles that contain lipid rafts (297). These actin
structures require activation of Arp2/3 and contain dynamin 2 (261, 297). Although the actin “comets” produced
in cells overexpressing PIP5KIB are exaggerated structures, a similar polymerization of actin has been observed
on endosomes in Xenopus eggs and in cultured mast cells
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core vesicle fusion by activating a PIP5KI enzyme in a
calcium-dependent manner (4). The calcium dependence
may be in part a protein kinase C (PKC)-regulated dephosphorylation of the PIP5KI, which activates it (4, 266, 382).
In the same cell type vesicle fusion is inhibited in cracked
cells incubated with recombinant C2A domains from various synaptotagmins, and this inhibition correlates with
the ability of the domain to bind to PtdIns(4,5)P2 (359).
Therefore, a synaptotagmin is likely to be one of the
effectors for PtdIns(4,5)P2 for membrane fusion at the
plasma membrane, at least for regulated secretion.
In the regulation of actin and the formation of clathrin-coated pits, it is clear that PtdIns(4,5)P2 increases the
affinity of many mutually interacting proteins for membranes. As such, it may participate in defining the membrane location for the events that require these proteins.
The AP2 adaptor, which binds membrane protein cargo to
the clathrin lattice, contains two binding sites for PIPs. In
the crystal structure of soluble AP2 core complex, these
sites are orthogonal to each other and could not simultaneously bind to the membrane (55). In this structure, the
binding pocket for internalization signals on receptors is
occluded. Owen and colleagues (55) have proposed that
binding to PIPs facilitates a conformational change that
opens the signal-binding pocket and allows both PI binding sites to face the membrane. This change may be
regulated by phosphorylation and the open conformation
stabilized by binding to PIPs. Mutation of the PIP binding
site on the AP2␣ subunit inhibits membrane binding, and
mutation of the binding site on the AP2␮ subunit prevents
binding to cargo, demonstrating the importance of the
interaction with PIPs (111, 291). AP2 can bind multiple
PIPs, and in vitro those with D-3 phosphate increase the
affinity of AP2 complexes for peptides that have internalization signals (286). This may be relevant to the observations that PtdIns3KIIC2␣ localizes in clathrin-coated
pits (112) and that PtdIns(3,4,5)P3 is important for recruitment of AP2 to activated ␤-adrenergic receptors (248).
However, given the relative scarcity of PtdIns(3,4,5)P3,
PtdIns(3,4)P2, and PtdIns(3)P at the plasma membrane, it
is likely that PtdIns(4,5)P2 is the major regulator of AP2
for constitutive endocytosis. The less abundant PIPs may
be generated as part of the signaling of hormone receptors and function locally to accelerate the internalization
of those receptors. Expression of PH domains specific for
PtdIns(4,5)P2 inhibits both early and late stages of clathrin-coated vesicle formation (171), and increased or decreased expression of PIP5KIB causes more or less AP2
to bind to membranes (262). In addition to AP2, a number
of other proteins important for endocytosis either have
been shown to bind PIPs or are recruited to membranes in
response to proteins that bind PIPs. The number of clathrin-coated pits at the plasma membrane and internalization of transferrin receptors increases or decreases in
direct relation to the production of PtdIns(4,5)P2 in sev-
713
714
MICHAEL G. ROTH
B. PtdIns(3)P on Endosomes
Clathrin-coated vesicles rapidly uncoat and fuse with
each other or with early endosomes. Although
PtdIns3KIIC2␣ has been found in clathrin-coated pits and
might still be present in vesicles when they uncoat, it is
not known if PtdIns(3)P is generated on the membrane of
incoming endocytic vesicles. In the presence of the PI3K
inhibitor wortmannin, internalization is either unaffected
or increased, and incoming endocytic vesicles continue to
fuse into structures larger than small vesicles. Thus, in the
absence of PtdIns(3)P, the incoming endocytic vesicles
are still competent for fusion. The effect of wortmannin is
to reduce the rate of entry of proteins into either the
recycling pathway back to the plasma membrane or the
pathway to late endosomes that leads to degradation in
lysosomes (166, 220, 321, 329). A number of observations
suggest that PtdIns(3)P is probably generated on the surface of early endosomes and not on the incoming vesicles
and that this difference may be used to give directionality
to the fusion reaction and to recruit the endosomal sorting machinery.
Wortmannin concentrations that inhibit PtdIns3KIII
inhibit the fusion of endosomes in vitro (166, 203, 329), a
reaction that requires activated Rab5. Activated Rab5
binds to a complex of proteins that includes PtdIns3KIII,
syntaxins, and accessory proteins that may play a role in
activating SNARE protein complexes for membrane fusion (225, 348). The effect of wortmannin on endosome
fusion in vivo is not bypassed by a constitutively active
Rab5, so the inhibited step is downstream of the guanine
nucleotide exchange on Rab5 required to deliver it to
membranes (167). A number of the effectors of Rab5
Physiol Rev • VOL
(EEA1, rabenosyn-5) bind PtdIns(3)P and are released
from membrane in the absence of this lipid (255, 270,
325). In an examination of the heterotypic fusion of uncoated endocytic vesicles with endosomes, Zerial and
colleagues (298) found Rab5 on each population of vesicle but found the Rab5 effector EEA1 only on early endosomes. EEA1 binds to membranes through a combination of interactions with PtdIns(3)P and other proteins
(88) but does not require a direct interaction with Rab5
for this (194). Thus a possible role of PtdIns(3)P on
endosomes that is consistent with the data just described
would be to identify the destination membrane for fusion
of incoming vesicles to give directionality to the fusion
reaction (298). Presumably, PtdIns(3)P would accomplish
this through the assembly of a protein complex on the
endosomes that would tether the incoming vesicle as well
as participate in the following fusion reaction. If this is
true, then the incoming endocytic vesicles should lack
PtdIns(3)P and a key determinant of endosome identification would therefore be the activation of a PtdIns3K.
Consistent with this proposal, PtdIns3KIII generates
PtdIns(3)P on phagosomes only after they have budded
off from the plasma membrane, and this is required for
them to fuse with lysosomes (366).
PtdIns(3)P is also important for a second step in
endocytic traffic, the formation of the internal vesicles of
MVEs. The endocytic pathway delivers to lysosomes most
of its luminal volume but only a minor fraction of its
membrane. The delivery of membrane proteins to lysosomes is therefore an active event, and the delivery of
fluid-phase cargo to lysosomes is the default outcome.
Proteins destined to be degraded, such as the epidermal
growth factor receptor (EGFR) bound to its ligand, are
sorted into regions on MVEs that bud off as internal
vesicles and therefore partition with luminal content to
lysosomes. The formation of these internal vesicles has a
topology opposite to the formation of other types of transport intermediates in the cell. Other transport vesicles
form when a cytosolic coat binds to a membrane, collects
cargo, and induces or stabilizes positive membrane curvature. After the vesicle fissions from the donor membrane (a process which is not understood), the peripheral
membrane proteins that form the coat are released back
into the cytosol to be reused (331). However, if the invaginations that form the internal vesicles in MVEs require a cytosolic coat to collect cargo and curve membrane, that coat will be incorporated in the interior of the
vesicle and be delivered to lysosomes for degradation. As
an alternative mechanism, protein coats may form on the
limiting membrane of MVEs to stabilize it, and the internal
vesicles might be formed by generating patches of lipid in
the cytoplasmic leaflet of uncoated membrane that favor
negative curvature and cause the membrane to invaginate
(275). The internal vesicles of MVEs are enriched in cholesterol and lysobisphosphatidic acid (186, 187, 241), in-
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(230, 349). The polymerization of actin appears to move
the organelles on which it is bound, but it is not clear if
this process is used to move vesicles in cells or actin
polymerization plays some other role.
Experiments in which the 5-phosphatase synaptojanin is deleted prove that there must be turnover of the
PtdIns(4,5)P2 on clathrin-coated vesicles for normal rates
of vesicle uncoating to occur. As mentioned previously,
synaptojanins are dual function phosphatases capable of
converting PtdIns(4,5)P2 to PtdIns without producing
PtdIns(4)P. In fact, at steady-state, a GFP-oxysterol binding protein PH domain probe or anti-PtdIns(4)P antibody
does not label the plasma membrane, suggesting that very
little free PtdIns(4)P2 is present there (372). Because
PtdIns(4)P is the precursor to PtdIns(4,5)P2, either it is
generated from PtdIns by a plasma membrane PtdIns4K,
such as PtdIns4KII␤ (377), directly at the site where it is
converted to PtdIns(4,5)P2, or it might be generated at the
Golgi but be rapidly converted to PtdIns(4,5)P2 upon arrival at the plasma membrane.
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
Physiol Rev • VOL
binding modules. One of these is the protein defective in
a S. cerevisiae class E vacuolar sorting mutant, Vps27
(274). Class E mutants inhibit the endocytic pathway at or
downstream of the point where proteins internalized from
the plasm membrane and proteins traveling from the
Golgi to the vacuole converge. The mammalian counterpart to Vps27, Hrs (188), forms a complex with STAM1,
STAM2, and eps15 (10). Hrs recruits clathrin to early
endosome membranes (281), and areas of flat clathrin
lattices are observed on endosomes that contain receptors destined to be degraded (281). Hrs interacts with the
PX domain-containing protein SNX1 and functions to sort
receptors from the recycling pathway into the internal
vesicles in MVEs for delivery to lysosomes (45, 280, 281).
Vps27p functions analogously in yeast (22). Thus Hrs
plays an early role as part of the sorting event in which
receptors are segregated from recycling proteins and
membrane into coated regions on early endosomes as
well as a later role when receptors are subsequently transferred to MVE vesicles. Hrs and Vps27p contain ubiquitin
interaction domains and are themselves monoubiquitylated. Many cell surface receptors are ubiquitylated at the
plasma membrane, and this serves as a signal that they
should be sorted into the degradative pathway after internalization rather than recycling to the plasma membrane
(138, 301, 337, 374). SNX1 binds to the EGFR, and overexpression of SNX1 increases the degradation of the receptor (192), whereas overexpression of Hrs inhibits
EGFR degradation (45, 189). This suggests that Hrs might
function to deliver a SNX1-EGFR complex into the
STAM1, STAM2, eps15 complex necessary for sorting.
The inhibition of EGFR degradation by overexpressed
Hrs may be due to free Hrs binding SNX in competition
with the Hrs that is part of the sorting complex. Three
additional multiprotein complexes on the same endosome
membrane are required for receptor degradation (176).
The order in which these complexes act has been determined through yeast genetics, but their functions are still
unclear.
C. PtdIns(3,5)P2 on MVEs/Vacuoles
The third protein with a PtdIns(3)P2 binding motif
that is necessary for generating the internal vesicles of
MVEs is the PtdIns(3)P 5-kinase, Fab1p/PIKfyve. The phenotype of ⌬fab1 yeast is similar to the phenotype in
mammalian cells in which PtdIns3KIII is inhibited (258),
suggesting that the invagination of MVE vesicles requires
production of PtdIns(3,5)P2. Interestingly, the PX domain
of SNX1 binds to both PtdIns(3)P and PtdIns(3,5)P2 on
liposomes (65); thus SNX1 may sort the EGFR into the
membrane domain that will become an internal MVE
vesicle.
PtdIns(3,5)P2 was first discovered in yeast subjected
to osmotic shock and then detected in mammalian cells
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dicating that sorting of lipids does occur during their
formation.
Several laboratories have used wortmannin to investigate the participation of PtdIns(3)P in the process of
forming MVE vesicles with somewhat contradictory results (26, 101, 109). A major problem for interpreting the
results of experiments that use wortmannin (and most
other inhibitors) in different cell types is that information
about the sensitivity of that particular cell to the inhibitor
is rarely provided. Because cells differ greatly in their
ability to inactivate drugs, the fact that an inhibitor has a
certain potency in vitro, or in a particular cell type, does
not mean that it has a similar potency in a different cell
type or over a different time course. A particularly instructive example of this is provided by Kundra and Kornfeld (191), who document that even a micromolar concentration of wortmannin is degraded in L cells fast
enough that inhibition of membrane traffic over a 3-h time
course requires addition of fresh drug at hourly intervals
(191). A second problem is that, in a number of different
cell types, at concentrations above 100 nM wortmannin
inhibits PtdIns3KIII, PtdIns3KIIC2␣, and PtdIns4KII␤ and
at low nanomolar concentration inhibits a phospholipase
A2 activity in Swiss 3T3 cells (68).
With these caveats in mind, 100 nM wortmannin inhibited the formation of MVE internal vesicles in a melanoma cell line (101). However, the recycling of proteins
from the limiting membrane of MVEs, but not the production of internal vesicles, was inhibited in NRK cells
treated with 200 nM wortmannin (26). Futter et al. (109)
investigated this question in experiments in which fusion
of MVEs with lysosomes was prevented and the drug was
added after a probe (EGFR) had passed through early
endosomes so that the process of formation of MVE vesicles could be uncoupled from effects on earlier or later
events. Under these conditions, HEp-2 cells treated with
200 nM wortmannin or microinjected with antibodies to
PtdIns3KIII contained fewer MVE internal vesicles containing EGFR and increased limiting membranes of swollen vacuoles carrying EGFR. The increase in the limiting
membrane was greater than would be predicted by the
decrease in the formation of the internal vesicles (109).
This suggests that PtdIns(3)P is important both for the
formation of internal MVE vesicles and for recycling
membrane from multivesicular endosomes back to recycling endosomes or other destinations. Consistent with
this interpretation, wortmannin has been reported to inhibit transport of mannose 6-phosphate receptors from
endosomes to the Golgi, as well as transport between
MVEs and lysosomes (191, 287). In contrast, Nakajima
and Pfeffer (252) report no inhibition of mannose 6-phosphate transport from endosomes to the TGN by wortmannin or another inhibitor of PtdIns3K, LY294002 (252).
Three proteins that function for sorting endocytic
cargo into the internal vesicles of MVEs have PtdIns(3)P
715
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MICHAEL G. ROTH
to the Golgi (191) raised the possibility that the inhibition
of Golgi sorting was due to a failure to recycle important
proteins back to the Golgi from endosomes. A second
complication for interpretation of the result that wortmannin inhibits sorting in the Golgi was the discovery that
overexpression of an enzymatically defective PtdIns3KIII
blocks delivery of cathepsin D to lysosomes but does not
cause it to be missorted at the Golgi, whereas treating
HeLa cells with 100 nM wortmannin causes both (296).
Wortmannin at that concentration might inhibit both
PtdIns3KIIC2␣ and PtdIns4KIII␤ (Table 1). Thus there is
currently no conclusive evidence that PtdIns3KIII functions at the Golgi, and the preponderance of evidence
suggests that this enzyme functions mainly on endosomes. A second PtdIns3K, PtdIns3KIIC2␣, has been reported to be associated with clathrin-coated vesicles on
the TGN, and its overexpression disrupts the intracellular
location of M6PR and lysosomal membrane proteins (80,
112). Clathrin/AP1 vesicles carry M6PRs from the Golgi to
endosomes and back (83, 141), and it is not known where
in this pathway PtdIns3KIIC2␣ is active. A protein of
novel function containing two FYVE domains binds to the
Golgi and when overexpressed can disrupt Golgi structure (290). However, the Golgi binding domain of this
protein is not found in the FYVE domain (44). The question of whether PtdIns(3)P plays any direct role in membrane traffic at the Golgi is currently unanswered.
D. PtdIns(3)P on the Golgi
E. PtdIns(4)P and PtdIns(4,5)P2 on the Golgi
VPS34 was identified in a screen for genes that when
mutated would allow vacuolar proteins to be secreted and
was subsequently found to encode a new PtdIns3K (312,
333, 367). Since the branch point in the biosynthetic pathway separating vacuolar proteins and secreted proteins
was the sorting event in the TGN, it was suspected that
Vps34p and its mammalian orthologs would function at
the Golgi. PtdIns3K inhibitors were found to disrupt the
sorting of lysosomal proteins in the Golgi, and this was
interpreted to mean that the site of PtdIns3K action was
the TGN (31, 72). A PtdIns3K activity was found to be
required for budding of vesicles containing the polyimmunoglobulin receptor from isolated rat hepatocyte Golgi
membranes (169), and wortmannin was observed to inhibit the sorting of mannose 6-phosphate receptors
(M6PRs) into vesicles, but not the budding of vesicles,
from the TGN (110). Wortmannin treatment also altered
the morphology of the TGN (139). The conclusion that the
effects of inhibiting PtdIns3Ks occurred on the Golgi began to be questioned when it was discovered that GFPFYVE domains labeled endosomes but not the Golgi (32,
118), suggesting that there is little free PtdIns(3)P on the
Golgi and the TGN. The observation that wortmannin
inhibited the movement of M6PRs from endosomes back
In a recent study of the cellular location of
PtdIns(4,5)P2, Watt et al. (375) used electron microscopy
and a PLC␦1-PH domain probe to quantify PtdIns(4,5)P2
on cellular membranes. After correcting for the fraction
of total membrane represented by each compartment, the
highest density of labeling was at the plasma membrane,
and the density of labeling of the Golgi was detectable but
ninefold lower than at the plasma membrane (375). Thus
the pool of free PtdIns(4,5)P2 on the Golgi is relatively
small. Interest in a possible role for PtdIns(4,5)P2 on the
Golgi arose when it was discovered that nucleotide exchange on the important regulator of Golgi membrane
traffic, Arf1, was increased by membranes containing
PtdIns(4,5)P2 (354) and that Arf is an activator of PLD
(29). PLD produces PA, which is a potent activator of all
of the PIP5KI enzymes, and PLD is itself potently stimulated by PtdIns(4,5)P2 (326). Thus the possibility that
secretory events on the Golgi might be regulated through
PtdIns(4,5)P2 acting in positive and negative feedback
mechanisms affecting Arf1 activity has received much
attention. Arf1 is a major regulator of membrane traffic at
the Golgi (293). There are six Arf proteins, and they can
be grouped into three families according to their sequence
relationships. Arfs 1, 2, and 3 are found at the Golgi (as
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(84, 384). Yeast (Fab1, Refs. 57, 226) and mammalian cells
(PIKfyve, Ref. 306) contain a single PtdIns(3)P 5-kinase
that produces PtdIns(3,5)P2. The FYVE domain of PIKfyve
is required for it to bind to endosomes (308). In S. cerevisiae, Vac14 is a regulator of Fab1 (24, 85). The mechanism
of this regulation is not known; however, in large scale
two-hybrid screens of the yeast genome, Vac14 has been
shown to interact with 17 other yeast proteins, including
proteins that interact with microtubules and components
of an oligomeric complex that binds to the Golgi (details
can be found at the Stanford Genomic Resources website).
PtdIns(3)P, and presumably PtdIns(3,5)P2, incorporated into the internal vesicles of MVEs is hydrolyzed
when these vesicles are transferred to the lumen of lysosomes or the yeast vacuole (395). However, there are
several cytosolic phosphatases in yeast and mammalian
cells capable of hydrolyzing PtdIns(3,5)P2 to PtdIns. Such
an activity would be needed if the spatial segregation of
these two lipids were controlled dynamically by degrading excess or free PtdIns(3,5)P2. Sac1 has PtdIns(3,5)P2
phosphatase activity, but complementation studies in
yeast suggest that it acts mainly on PtdIns(4)P (20).
MTMR1, MTMR2, MTMR3, and MTMR6 hydrolyze both
PtdIns(3)P and PtdIns(3,5)P2 and are candidates for activities that control the levels of those lipids in the limiting
membranes of organelles in mammalian cells (20, 309).
PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
Physiol Rev • VOL
back to PtdIns(4)P. Another possibility is the remarkable
observation that a kinesin, unc104/KIF1A, binds preferentially to vesicles containing PtdIns(4,5)P2 (185). The ability of unc104/KIF1A to move vesicles is sharply dependent
on the concentration of PtdIns(4,5)P2, and if that lipid is
generated at the site of vesicle budding to recruit and
activate a motor, PtdIns(4,5)P2 might be rapidly exported
with the vesicle, keeping the pool of free PtdIns(4,5)P2 on
the Golgi low. The concentration of PtdIns(4,5)P2 required to activate the motor is lowered when raft-forming
lipids are added to the vesicles (185). This suggests that
raft lipids, cholesterol and glycospingolipids, may serve to
concentrate PtdIns(4,5)P2 and enhance binding of the
vesicle to the motor. Both polarized and nonpolarized
cells contain separate raft and nonraft pathways from the
Golgi (247, 406). It is an interesting possibility that raft
and nonraft transport pathways may recruit different PI
kinases, differ in the phosphoinositide that they employ,
and perhaps the motors that associate with them.
F. Phosphoinositides on the ER
In contrast to the other organelles involved in membrane traffic, there is very little indication that PIPs play a
direct role in constitutive traffic from the ER to the Golgi.
The ER and nuclear membrane contain ⬃10% of the cellular PtdIns(4,5)P2 labeled with a PH domain probe (375).
The COPII coat responsible for membrane protein export
from the ER preferentially binds to acidic phospholipids
but does not show a preference for specific PIPs (221).
Several PI kinases and phosphatases are located on the
ER, but the exact role that they play in secretion, if any, is
not known (224, 389, 392). Membrane traffic between the
ER and Golgi is inhibited when PtdOH production by PLD
is blocked (21, 322), but it is not clear if this is an effect
on the ER or the Golgi.
V. SUMMARY AND CONCLUSIONS
Previous sections have summarized data indicating
that proteins that make, consume, and bind to PIPs are
important for constitutive membrane traffic. Different
PIPs are concentrated in different parts of the central
vacuolar pathway, with PtdIns(4)P predominate on Golgi,
PtdIns(4,5)P2 predominate at the plasma membrane,
PtdIns(3)P the major PIP on early endosomes, and
PtdIns(3,5)P2 found on late endocytic organelles. The
reason for this spatial segregation is not known but may
be the mechanism by which the direction of membrane
traffic is controlled. One problem for organization within
the central vacuolar system is to establish the identity of
dynamic organelles that are constantly exchanging membranes. The integral membrane components that function
for membrane traffic, including cargo receptors and mem-
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well as elsewhere in the cell) where they regulate the
formation of COPI and clathrin-coated vesicles and are
required for many secretion events. Arf6 functions at the
plasma membrane to regulate actin and a non-clathrinmediated endocytic pathway. No step in membrane traffic
specifically requiring Arf4 or -5 has been reported. A
number of the guanine nucleotide exchange factors
(GEFs) and GTPase accelerating proteins (GAPs) for
Arfs, as well as other proteins involved in Golgi membrane traffic, bind PtdIns(4,5)P2 or PA (30, 174, 215, 265,
284, 285). Arf1 is a direct activator of both PIP5KIB and
PI4KII␤ and stimulates the production of PtdIns(4,5)P2 on
Golgi membranes in vitro (120, 168). Golgi membranes
isolated from cells overexpressing PLD1 show elevated
production of PtdIns(4,5)P2 (294), consistent with stimulation of a PIP5KI enzyme by PA. In a series of studies,
Shields and colleagues (322, 323, 346) have shown that
PtdIns(4,5)P2 is required to maintain Golgi structure and
its production is regulated through the production of PA.
Overexpression of a dominant negative PI4KII␤ disrupts
the structure of the Golgi, perhaps by interfering with the
ability of spectrin to bind to membranes (120), although it
is not clear if this is due to the lack of a precursor for
PtdIns(4,5)P2 or to a direct effect of insufficient
PtdIns(4)P. The release of secretory vesicles exporting
hormones from the TGN requires PtdIns(4,5)P2 (42, 324).
The nature of the vesicle coat, if any, involved in this
transport step is not known. AP1/clathrin coats are
thought to sort and transport a number of proteins from
the TGN. The AP1 clathrin adaptor has been shown to
bind to liposomes in a manner that requires Arf1 and
cargo with tyrosine signals and is facilitated by
PtdIns(4,5)P2 more than by any other PI (69).
However, PtdIns(4)P is the major phosphoinositide
on Golgi membranes and has functions independent of its
use as a precursor for PtdIns(4,5)P2 (201, 372). In yeast,
membrane traffic through the Golgi requires PtdIns(4)P
generated by Pik4 (9, 338) and does not require
PtdIns(4,5)P2. Yin and colleagues (372) found that
PtdIns(4)P was the major lipid on mammalian Golgi membranes and inhibition of PI4KII␣ by small interfering RNA
caused the Golgi to fragment and inhibited the export of
a viral glycoprotein from the TGN. The binding of AP1 to
Golgi membranes was lost in these cells. AP1 binding and
Golgi fragmentation were rescued by adding PtdIns(4)P
back to cells but not by adding PtdIns(4,5)P2 (372). However, the inhibition of glycoprotein export was rescued by
both lipids. Thus PtdIns(4)P functions in maintaining
Golgi structure both directly and through conversion to
PtdIns(4,5)P2, probably by recruiting cytoskeleton to
Golgi membranes and by maintaining the flux of membrane moving through the organelle. One explanation for
why PtdIns(4,5)P2 levels might be relatively low on Golgi
membranes is that the 5-phosphatase OCRL on that organelle (87) might rapidly convert Golgi PtdIns(4,5)P2
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MICHAEL G. ROTH
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PHOSPHOINOSITIDES IN MEMBRANE TRAFFIC
abundant enough to allow weak interaction with most of
the proteins that bind to them, which have dissociation
constants in the 10 ␮M range. This weak binding means
that interactions will be extremely brief (less than milliseconds) unless stabilized by additional interactions.
Many, if not most, PIP binding proteins have multiple PIP
binding sites either on the same polypeptide or because
they oligomerize, and these proteins usually also bind to
other proteins on the membrane. Thus stable binding can
be achieved through increases in avidity that occur as
proteins binding weakly to the PIP on the membrane find
and bind to each other. This allows a situation where once
a critical concentration of PIP is generated a multimeric
complex of proteins can assemble, and the stability of the
complex can be controlled by the concentration of the
PIP in the membrane. Since the cytosolic coats on transport intermediates need to assemble and then disassemble, some sort of cycling between active and inactive
states is required. This occurs at multiple levels, including
GTP hydrolysis on Rab and Arf proteins as well as phosphorylation of the membrane protein components and the
lipids. Thus the formation of a vesicle coat or the docking
and fusion of a vesicle are similar to a logical coincident
gate. If multiple events do not coincide on the relevant
time scale (which is determined by the affinity of mutually
interacting components and their local concentration),
then the traffic machinery will disassemble and start over
again. This combinatorial approach is used in membrane
traffic as a proofreading function that preserves the individual identities of highly fluid membranous organelles.
Address for reprint requests and other correspondence:
M. G. Roth, Dept. of Biochemistry, Univ. of Texas Southwestern
FIG. 2. A model for the role of phosphoinositides in the formation of membrane transport intermediates. A: in the
off state, phosphoinositide concentrations are below a required threshold. Membrane cargo is dispersed and elements
that will nucleate the formation of a transport intermediate are binding with low affinity to membranes, remaining largely
in the cytosol. One of these components binds to the major phosphoinositide found at this site, and one binds to cargo.
Although these components are shown here as separate entities, they could be separate modules on the same protein.
Other postulated components are a small GTP-binding protein and a PI kinase. B: the cargo-binding protein and
PI-binding protein interact, possibly due to a conformational change induced by the binding to PI. This decreases their
off rate, and they remain longer at the membrane, increasing the chance that they will interact with the other components
that are binding independently to the membrane. C: GTP exchange occurs on the small G protein, through interaction
with one of the first two components or a separate exchange factor (not shown). The small G protein activated by GTP
binds tightly to the membrane and stabilizes the first two components as well as activates a PI-kinase and/or other
lipid-modifying enzymes. Only if all components are present during the period defined by their collective binding affinity
to the membrane will a productive complex form that can grow into a membrane coat. D: the increased stability of the
first four components as well as a local increase in PI concentration allows stable binding of additional PI- and cargo
binding components that interact and serve to collect cargo into the growing patch of coated membrane. E: an additional
layer of coat structural components (such as clathrin) stabilizes the coat complex. The expansion of the coat requires
cycles of guanine nucleotide exchange by the small G protein, presumably so that it can release from coat subunits to
allow them to interact. The structural components bring in additional regulators such as a PI-phosphatase and possibly
a PI-kinase kinase (not shown). F: growth of the coat is limited by hydrolysis of the PI to PtdIns, by termination of
guanine nucleotide exchange on the small G protein and release or inhibition of the PI-kinase. G: the events that form
the highly curved narrow membrane neck that must proceed vesicle fission are not understood. Changing lipid species
to promote the required membrane curvature could help. Motor proteins pulling on the vesicle or actin polymerization
around the neck could add mechanical force for membrane fission. H: the transport intermediate uncoats through
addition of a destabilizing force during or after fission, facilitated by the weakened membrane binding caused by the loss
of PI through the action of the PI-phosphatase.
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brane docking and fusion machinery, shuttle back and
forth between organelles. To establish vectorial transport,
this machinery must be activated only at the correct site
and subsequently inactivated during recycling processes
when proteins are transported back to the site where they
function. The cytosolic coat proteins that recognize these
components during the sorting process that loads them
into transport intermediates must recognize them only at
the correct membrane. A way to achieve this is to transiently increase the affinity of an area of membrane for
these cytosolic proteins by modifying the lipids. In a
process analogous to the phosphorylation of proteins,
phosphorylation and dephosphorylation of PIPs could
serve to switch a membrane from an active to an inactive
state (Fig. 2).
If, for the sake of argument, one accepts that PIPs
serve as organelle markers for membrane transport machinery, how do they become concentrated on the correct
membrane? It is clear that the local concentration of PIPs
is controlled dynamically by the balance between the
kinases that make them and the phosphatases that hydrolyze them, since overexpression of the kinases or deletion
of the phosphatases causes the distribution of PIPs to
change. This raises the question of how the activity of the
kinases and phosphatases is regulated at the correct location. We are currently far from understanding this process, but it is one of the most important problems for
understanding how membrane traffic is organized.
Another important question is how PIPs serve as
membrane identifiers. Here we have a few clear answers.
One clue is the relatively weak binding between PIPs and
the protein modules selective for them. PtdIns(3)P,
PtdIns(4)P, and PtdIns(4,5)P2 are each ⬃5 mol% of the
cytoplasmic leaflet where they are concentrated, which is
719
720
MICHAEL G. ROTH
Medical Center at Dallas, 5323 Harry Hines Blvd., Dallas, TX
75390-9038 (E-mail: [email protected]).
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