激动剂诱导受体激活的动力学。
Dynamics of receptor activation by agonists.
机构信息
Department of Physiology and Biophysics, State University of New York at Buffalo, Buffalo, New York.
出版信息
Biophys J. 2024 Jul 16;123(14):1915-1923. doi: 10.1016/j.bpj.2024.01.003. Epub 2024 Jan 4.
Abstract
How do agonists turn on receptors? The model system we have used to address this question is the adult-type skeletal muscle nicotinic acetylcholine receptor. This ligand-gated ion channel has two orthosteric sites (for neurotransmitters) in the extracellular domain linked to an allosteric site (a gate) in the transmembrane domain. The goal of this perspective is to summarize how measurements of agonist binding energy reveal the dynamics of the neurotransmitter sites and the fundamental link between binding and gating.
摘要
激动剂如何开启受体？我们用来解决这个问题的模式系统是成年型骨骼肌烟碱型乙酰胆碱受体。这种配体门控离子通道在细胞外域有两个正位（神经递质）结合位点，与跨膜域的别构（门）位点相连。本观点的目的是总结激动剂结合能的测量如何揭示神经递质位点的动力学以及结合与门控之间的基本联系。
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