Molecular Determinants Conferring the Stoichiometric-Dependent Activity of α-Conotoxins at the Human α9α10 Nicotinic Acetylcholine Receptor Subtype,Journal of Medicinal Chemistry

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Molecular Determinants Conferring the Stoichiometric-Dependent Activity of α-Conotoxins at the Human α9α10 Nicotinic Acetylcholine Receptor Subtype
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2018-05-07 00:00:00 , DOI: 10.1021/acs.jmedchem.8b00115
Rilei Yu _{1,

2} , Han-Shen Tae ₃ , Nargis Tabassum _{1,

2} , Juan Shi _{1,

2} , Tao Jiang _{1,

2} , David J. Adams ₃

Affiliation

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.

中文翻译：

分子决定簇赋予α-芋螺毒素在人α9α10烟碱乙酰胆碱受体亚型的化学计量比活性

推测α9α10烟碱乙酰胆碱受体（nAChRs）存在于不同的化学计量比中。我们系统地研究了在人α9α10nAChR的假设化学计量比下，α-芋螺毒素Vc1.1，RgIA＃和PeIA抑制的分子决定因素。我们的结果表明，只有Vc1.1对α9α10nAChR表现出化学计量依赖性。在α9（+）-α9（-）界面处，α9的N154和Vc1.1的D11之间的氢键负责Vc1.1的化学计量依赖性。

更新日期：2018-05-07

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