NDLI: Size matters in activation/inhibition of ligand-gated ion channels

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Size matters in activation/inhibition of ligand-gated ion channels

Content Provider	PubMed Central
Author	Du, Juan Dong, Hao Zhou, Huan-xiang
Copyright Year	2012
Abstract	Cys-loop, glutamate, and P2X receptors are ligand-gated ion channels (LGICs) with 5, 4, and 3 protomers, respectively. There is now growing atomic-level understanding of their gating mechanisms. Although each family is unique in the architecture of the ligand-binding pocket, the pathway for motions to propagate from ligand-binding domain to transmembrane domain, and the gating motions of the transmembrane domain are similar. Here we review common features among the LGICs. In particular, agonists and competitive antagonists apparently induce opposite motions of the binding pocket. A simple way to control the motional direction is ligand size. Agonists, usually small, induce closure of the binding pocket, leading to opening of the channel pore, whereas antagonists, usually large, induce opening of the binding pocket, thereby stabilizing the closed pore. A cross-family comparison of the gating mechanisms of the LGICs, focusing in particular on the role played by ligand size, provides new insight on channel activation/inhibition and design of pharmacological compounds.
Related Links	http://dx.doi.org/10.1016/j.tips.2012.06.005
Ending Page	493
Page Count	12
Starting Page	482
File Format	PDF
ISSN	01656147
e-ISSN	18733735
Journal	Trends in pharmacological sciences
Issue Number	9
Volume Number	33
Language	English
Publisher Date	2012-09-01
Access Restriction	Open
Subject Keyword	Toxicology Pharmacology Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Toxicology Pharmacology

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