RIS ID

128183

Publication Details

Yu, R., Tae, H., Tabassum, N., Shi, J., Jiang, T. & Adams, D. J. (2018). Molecular Determinants Conferring the Stoichiometric-Dependent Activity of α-Conotoxins at the Human α9α10 Nicotinic Acetylcholine Receptor Subtype. Journal of Medicinal Chemistry, 61 (10), 4628-4634.

Abstract

α9α10 nicotinic acetylcholine receptors (nAChRs) putatively exist at different stoichiometries. We systematically investigated the molecular determinants of α-conotoxins Vc1.1, RgIA#, and PeIA inhibition at hypothetical stoichiometries of the human α9α10 nAChR. Our results suggest that only Vc1.1 exhibits stoichiometric-dependent inhibition at the α9α10 nAChR. The hydrogen bond between N154 of α9 and D11 of Vc1.1 at the α9(+)-α9(−) interface is responsible for the stoichiometric dependent potency of Vc1.1.

Grant Number

ARC/DP150103990

Available for download on Tuesday, May 07, 2019

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