PMID: 9649383Jul 2, 1998Paper

Extrapore residues of the S5-S6 loop of domain 2 of the voltage-gated skeletal muscle sodium channel (rSkM1) contribute to the mu-conotoxin GIIIA binding site

Biophysical Journal
M ChahineR G Kallen

Abstract

The tetradomain voltage-gated sodium channels from rat skeletal muscle (rSkM1) and from human heart (hH1) possess different sensitivities to the 22-amino-acid peptide toxin, mu-conotoxin GIIIA (mu-CTX). rSkM1 is sensitive (IC50 = 51.4 nM) whereas hH1 is relatively resistant (IC50 = 5700 nM) to the action of the toxin, a difference in sensitivity of >100-fold. The affinity of the mu-CTX for a chimera formed from domain 1 (D1), D2, and D3 from rSkM1and D4 from hH1 (SSSH; S indicates origin of domain is skeletal muscle and H indicates origin of domain is heart) was paradoxically increased approximately fourfold relative to that of rSkM1. The source of D3 is unimportant regarding the difference in the relative affinity of rSkM1 and hH1 for mu-CTX. Binding of mu-CTX to HSSS was substantially decreased (IC50 = 1145 nM). Another chimera with a major portion of D2 deriving form hH1 showed no detectable binding of mu-CTX (IC50 > 10 microM). These data indicate that D1 and, especially, D2 play crucial roles in forming the mu-CTX receptor. Charge-neutralizing mutations in D1 and D2 (Asp384, Asp762, and Glu765) had no effect on toxin binding. However, mutations at a neutral and an anionic site (residues 728 and 730) in S5-S6/D2 of rSkM1, w...Continue Reading

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Citations

Nov 22, 2000·Biochimie·S Cestèle, W A Catterall
Jun 10, 2011·Proceedings of the National Academy of Sciences of the United States of America·Michael J WilsonMin-Min Zhang
Jun 19, 2009·The Journal of Biological Chemistry·Dewen YouRen Lai
Jan 5, 2002·The Journal of General Physiology·Kwokyin HuiRobert J French
Jul 2, 2003·The Journal of General Physiology·Kwokyin HuiRobert J French
Feb 6, 2014·Proceedings of the National Academy of Sciences of the United States of America·Joanna GajewiakMin-Min Zhang
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