Article
How batrachotoxin modifies the sodium channel permeation pathway: computer modeling and site-directed mutagenesis.
Molecular pharmacology - 1 Mar 2006
Wang Sho-Ya, Mitchell Jane, Tikhonov Denis B, Zhorov Boris S, Wang Ging Kuo
Abstract excerpt
A structural model of the rNav1.4 Na+ channel with batrachotoxin (BTX) bound within the inner cavity suggested that the BTX pyrrole moiety is located between a lysine residue at the DEKA selectivity filter (Lys1237) and an adjacent phenylalanine residue (Phe1236). We tested this pyrrole-binding model by site-directed mutagenesis of Phe1236 at D3/P-loop with 11 amino acids. Mutants F1236D and F1236E expressed...
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