Open channel blockade of AMPA receptors by philanthotoxins is influenced by alternate flip/flop splicing

P05
Open channel blockade of AMPA receptors by philanthotoxins is influenced by alternate flip/flop splicing
John William Grzeskowiak, Henrik Franzyk, Kristian Strømgaard, Ian R. Mellor
The University of Nottingham, School of Biology
‐9
Kainic acid
10
M
‐8
10
M
‐7
10
M
‐6
10
M
‐5
10
M
‐4
10
M
PhTX‐343
Pei et al; Biochemistry 2009, 48, 3767‐3777
Test Compounds
Site Directed Mutagenesis
PhTX‐343
PhTX‐343 (65)
PhTX‐343 (66)
Relative Position
Subunit
PhTX‐343 (67)
PhTX‐343 (68)
1 2 3 4
5 6 7 8 9
GluA1 flop
G A F M Q Q G C D
GluA1 flop Q601R
G A F M Q R G C D
GluA1 flop G602A
G A F M Q Q A C D
GluA1 flop C603S
G A F M Q Q G S D
GluA2 flop
G A F M R Q G C D