储存式钙通道的药理学
Pharmacology of store-operated calcium channels.
作者信息
Putney James W
机构信息
Calcium Regulation Section, National Institute of Environmental Health Sciences - NIH, Department of Health and Human Services, PO Box 12233, Research Triangle Park, NC 27709, USA.
出版信息
Mol Interv. 2010 Aug;10(4):209-18. doi: 10.1124/mi.10.4.4.
Abstract
Store-operated calcium entry is a process by which the depletion of calcium from the endoplasmic reticulum activates calcium influx across the plasma membrane. In the past few years, the major players in this pathway have been identified. STIM1 and STIM2 function as calcium sensors in the endoplasmic reticulum and can interact with and activate plasma membrane channels comprised of Orai1, Orai2, or Orai3 subunits. This review discusses recent advances in our understanding of this widespread signaling mechanism as well as the mechanisms by which a number of interesting pharmacological agents modify it.
摘要
钙库操纵性钙内流是一种内质网钙耗竭激活跨质膜钙内流的过程。在过去几年中，该信号通路中的主要分子已被鉴定出来。基质相互作用分子1（STIM1）和基质相互作用分子2（STIM2）作为内质网中的钙传感器，可与由Orai1、Orai2或Orai3亚基组成的质膜通道相互作用并激活这些通道。本文综述了我们对这一广泛存在的信号机制的最新认识进展，以及一些有趣的药理试剂对其进行调节的机制。
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Two novel 2-aminoethyl diphenylborinate (2-APB) analogues differentially activate and inhibit store-operated Ca(2+) entry via STIM proteins.两种新型 2-氨基乙基二苯硼酸盐（2-APB）类似物通过 STIM 蛋白差异激活和抑制储存操纵的 Ca(2+)内流。
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