本末倒置：配体激活通道反向变构调控的可能机制。
The tail wags the dog: possible mechanism for reverse allosteric control of ligand-activated channels.
作者信息
Vardy E, Kenakin T
机构信息
Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC, USA.
出版信息
Br J Pharmacol. 2014 Apr;171(7):1614-6. doi: 10.1111/bph.12550.
Abstract
In this issue of the British Journal of Pharmacology, a new article by Kozuska et al. discusses the multiple salt bridges in the intracellular domain of the 5HT3A receptor. These interactions increase the overall rigidity of the receptor, stabilize its low conducting state and affect the ligand cooperativity. The authors suggest that the allosteric effects of these regions on the receptor may be involved in a possible 'reverse' allosteric modulation of 5HT3 receptors.
摘要
在本期《英国药理学期刊》中，科祖斯卡等人撰写的一篇新文章探讨了5HT3A受体胞内结构域中的多个盐桥。这些相互作用增加了受体的整体刚性，稳定了其低传导状态，并影响配体协同性。作者认为，这些区域对受体的变构效应可能参与了5HT3受体一种可能的“反向”变构调节。
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本文引用的文献
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Physiology and pathophysiology of the 5-HT3 receptor.5-羟色胺3型受体的生理学与病理生理学
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