Binding of Ala-scanning analogs of ω-conotoxin MVIIC to N- and P/Q-type calcium channels
ω-Conotoxin MVIIC binds to P/Q-type calcium channels with high affinity and N-type channels with low affinity. To reveal the residues essential for subtype selectivity, we synthesized Ala-scanning analogs of MVIIC. Binding assays using rat cerebellar P 2 membranes suggested that Thr 11, Tyr 13 and L...
Saved in:
Published in | FEBS letters Vol. 469; no. 2; pp. 147 - 150 |
---|---|
Main Authors | , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
England
Elsevier B.V
10.03.2000
|
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | ω-Conotoxin MVIIC binds to P/Q-type calcium channels with high affinity and N-type channels with low affinity. To reveal the residues essential for subtype selectivity, we synthesized Ala-scanning analogs of MVIIC. Binding assays using rat cerebellar P
2 membranes suggested that Thr
11, Tyr
13 and Lys
2 are essential for binding to both N- and P/Q-type channels, whereas Lys
4 and Arg
22 are important for binding to P/Q-type channels. These results suggest that MVIIC interacts with P/Q-type channels via a large surface, in good agreement with previous observations using chimeric analogs. |
---|---|
ISSN: | 0014-5793 1873-3468 |
DOI: | 10.1016/S0014-5793(00)01263-1 |