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
收藏
页码：140 / 146
页数：7
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