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

被引：4

作者：

Skopin, A. Y. ^{[1
]}

Grigoryev, A. D. ^{[1
]}

Glushankova, L. N. ^{[1
]}

Shalygin, A., V ^{[1
]}

Wang, G. ^{[2
]}

Kartzev, V. G. ^{[3
]}

Kaznacheyeva, E., V ^{[1
]}

机构：

[1] Russian Acad Sci, Inst Cytol, St Petersburg 194064, Russia

[2] Soochow Univ, Coll Pharmaceut Sci, Suzhou 215123, Jiangsu, Peoples R China

[3] InterBioscreen Ltd, Chernogolovka 142432, Russia

来源：

ACTA NATURAE | 2021年 / 13卷 / 01期

基金：

俄罗斯科学基金会; 俄罗斯基础研究基金会;

关键词：

calcium; store-operated ca(2+) entry; STIM1; STIM2; 2-APB; Orai; 2-AMINOETHOXYDIPHENYL BORATE; CALCIUM-ENTRY; STIM2; INHIBITION; RECEPTOR; ORAI1; TRPC1; POTENTIATION; ANALOGS; SENSOR;

D O I：

10.32607/actanaturae.11269

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Store-opeated Ca2+ 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 Ca2+ sensors STIM1 and STIM2 are the key components of store-operated Ca2+ entry in mammalian cells. Under physiological conditions, STIM proteins are responsible for store-operated Ca2+ 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 Ca2+ entry (IC50 = 1 mu M) and had almost no effect on the STIM1-dependent activation of store-operated channels.

引用

页码：140 / 146

页数：7

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