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一种新型的STIM2依赖性钙库操纵性钙通道活性调节剂。

A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity.

作者信息

Skopin A Y, Grigoryev A D, Glushankova L N, Shalygin A V, Wang G, Kartzev V G, Kaznacheyeva E V

机构信息

Institute of Cytology of Russian Academy of Sciences, St. Petersburg, 194064 Russia.

College of Pharmaceutical Sciences, Soochow University, Suzhou, Jiangsu, 215123 China.

出版信息

Acta Naturae. 2021 Jan-Mar;13(1):140-146. doi: 10.32607/actanaturae.11269.

DOI:10.32607/actanaturae.11269
PMID:33959394
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8084296/
Abstract

Store-operated Ca entry is one of the main pathways of calcium influx into non-excitable cells, which entails the initiation of many intracellular processes. The endoplasmic reticulum Ca sensors STIM1 and STIM2 are the key components of store-operated Ca entry in mammalian cells. Under physiological conditions, STIM proteins are responsible for store-operated Ca entry activation. The STIM1 and STIM2 proteins differ in their potency for activating different store-operated channels. At the moment, there are no selective modulators of the STIM protein activity. We screened a library of small molecules and found the 4-MPTC compound, which selectively inhibited STIM2-dependent store-operated Ca entry (50 = 1 μM) and had almost no effect on the STIM1-dependent activation of store-operated channels.

摘要

钙库操纵性钙内流是钙流入非兴奋性细胞的主要途径之一，它引发许多细胞内过程。内质网钙传感器STIM1和STIM2是哺乳动物细胞中钙库操纵性钙内流的关键组成部分。在生理条件下，STIM蛋白负责激活钙库操纵性钙内流。STIM1和STIM2蛋白在激活不同钙库操纵性通道的能力上有所不同。目前，尚无STIM蛋白活性的选择性调节剂。我们筛选了一个小分子文库，发现了4-MPTC化合物，它能选择性抑制STIM2依赖性钙库操纵性钙内流（IC50 = 1 μM），而对STIM1依赖性钙库操纵性通道的激活几乎没有影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/49d3e5330af5/AN20758251-13-01-140-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/1430dbeb35ba/AN20758251-13-01-140-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/dd87ae0935f6/AN20758251-13-01-140-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/de848d4abee0/AN20758251-13-01-140-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/49d3e5330af5/AN20758251-13-01-140-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/1430dbeb35ba/AN20758251-13-01-140-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/dd87ae0935f6/AN20758251-13-01-140-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/de848d4abee0/AN20758251-13-01-140-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/871f/8084296/49d3e5330af5/AN20758251-13-01-140-g004.jpg

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