Canonical transient receptor potential 4 and its small molecule modulators

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• 作者：Jie Fu (1) (2)
  ZhaoBing Gao (2)
  Bing Shen (1)
  Michael X. Zhu (2) (3)
  
  1. Department of Physiology ; Anhui Medical University ; Hefei ; 230032 ; China
  2. International Scientist Workstation of Neuropharmacology ; Shanghai Institute of Materia Medica ; Chinese Academy of Sciences ; Shanghai ; 201203 ; China
  3. Department of Integrative Biology and Pharmacology ; the University of Texas Health Science Center at Houston ; Houston ; Texas ; 77030 ; USA
  
• 关键词：TRPC4 channel ; non ; selective cation channel ; G protein coupled receptors ; small molecular modulators ; G proteins ; excitation ; contraction ; Ca2+ signaling
• 刊名：Science China Life Sciences
• 出版年：2015
• 出版时间：January 2015
• 年：2015
• 卷：58
• 期：1
• 页码：39-47
• 全文大小：727 KB
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• 刊物主题：Life Sciences, general;
• 出版者：Springer Berlin Heidelberg
• ISSN：1869-1889

文摘

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.