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

A. Yu. Skopin | Zendy; Andrey D. Grigoryev | Zendy; Л. Н. Глушанкова | Zendy; Alexey Shalygin | Zendy; Guanghui Wang | Zendy; Viktor G. Kartzev | Zendy; Еlena Kaznacheyeva | Zendy

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

Author(s) -

A. Yu. Skopin,

Andrey D. Grigoryev,

Л. Н. Глушанкова,

Alexey Shalygin,

Guanghui Wang,

Viktor G. Kartzev,

Еlena Kaznacheyeva

Publication year - 2021

Publication title -

acta naturae

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.475

H-Index - 26

ISSN - 2075-8251

DOI - 10.32607/actanaturae.11269

Subject(s) - chemistry , orai1 , microbiology and biotechnology , biophysics , neuroscience , biology , biochemistry , stim1 , endoplasmic reticulum

Store-operated Ca 2+ 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 2+ sensors STIM1 and STIM2 are the key components of store-operated Ca 2+ entry in mammalian cells. Under physiological conditions, STIM proteins are responsible for store-operated Ca 2+ 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 2+ entry ( IC 50 = 1 μM) and had almost no effect on the STIM1-dependent activation of store-operated channels.

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