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Abstract
Results 2:
α-NETA Stability, Potential Bioactive
Degradation Products, and StructureActivity Relationships
Results 4:
α-NETA Suppresses Clinical and
Histological EAE: comparison with
FDA-approved Dimethyl Fumarate
Proposed Degradation Pathway of α-NETA
α-NETA
Dimethyl Fumarate (DMF)
242 Da
electrophile
144 Da
electrophile
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β
Graham et al, PLoS One 2014
Schilling et al, Clin and Expt Immunol 2006
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μ
α-
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μ
(A) Proposed Degradation Pathway of α-NETA (supported by MS-TOF data). (B)
α-NETA stability. α-NETA was spiked into 10% mouse plasma and incubated at
the indicated temperatures. At the indicated times, the samples were quenched
and analyzed by mass spectrometry. The stability of Benfluorex (positive control
compound) was also determined. Mean ± SD of triplicate wells for each point is
displayed. (C)
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Results 3: α-NETA Selectivity
Results 1:
α-NETA Selectively Inhibits CMKLR1 Signaling
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l2
chemerin
ga
α
b-
CMKLR1
b-a
rre
CHO cells
b-
stin
:b-g
ga
l2
al1
Chemilluminescent
Signal
β-arrestin:β-gal1
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Substrate
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β
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β
β
β
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Conclusions
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