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

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...

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Published in:Actanaturae Vol. 13; no. 1; pp. 140 - 146
Main Authors: Skopin, A Y, Grigoryev, A D, Glushankova, L N, Shalygin, A V, Wang, G, Kartzev, V G, Kaznacheyeva, E V
Format: Journal Article
Language:English
Published: Russia (Federation) A.I. Gordeyev 01-01-2021
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Summary: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.
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ISSN:2075-8251
DOI:10.32607/actanaturae.11269