Canonical transient receptor potential 4 and its small molecule modulators  被引量:4

Canonical transient receptor potential 4 and its small molecule modulators

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作  者:FU Jie GAO ZhaoBing SHEN Bing ZHU Michael X. 

机构地区:[1]Department of Physiology,Anhui Medical University [2]International Scientist Workstation of Neuropharmacology,Shanghai Institute of Materia Medica,Chinese Academy of Sciences [3]Department of Integrative Biology and Pharmacology,the University of Texas Health Science Center at Houston

出  处:《Science China(Life Sciences)》2015年第1期39-47,共9页中国科学(生命科学英文版)

基  金:supported in part by the National Natural Science Foundation of China(81228021);US National Institutes of Health(DK081654)

摘  要:Canonical transient receptor potential 4(TRPC4) forms non-selective cation channels that contribute to phospholipase C-dependent Ca2+ entry into cells following stimulation of G protein coupled receptors and receptor tyrosine kinases.Moreover,the channels are regulated by pertussis toxin-sensitive Gi/o proteins,lipids,and various other signaling mechanisms.TRPC4-containing channels participate in the regulation of a variety of physiological functions,including excitability of both gastrointestinal smooth muscles and brain neurons.This review is to present recent advances in the understanding of physiology and development of small molecular modulators of TRPC4 channels.Canonical transient receptor potential 4(TRPC4) forms non-selective cation channels that contribute to phospholipase C-dependent Ca^2+ entry into cells following stimulation of G protein coupled receptors and receptor tyrosine kinases.Moreover,the channels are regulated by pertussis toxin-sensitive Gi/o proteins,lipids,and various other signaling mechanisms.TRPC4-containing channels participate in the regulation of a variety of physiological functions,including excitability of both gastrointestinal smooth muscles and brain neurons.This review is to present recent advances in the understanding of physiology and development of small molecular modulators of TRPC4 channels.

关 键 词:TRPC4 channel non-selective cation channel G protein coupled receptors small molecular modulators G proteins EXCITATION CONTRACTION Ca2+ signaling 

分 类 号:Q257[生物学—细胞生物学] TQ326.5[化学工程—合成树脂塑料工业]

 

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