Title of article
A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
Author/Authors
Skopin, A.Y Institute of Cytology of Russian Academy of Sciences, St. Petersburg, Russia , Grigoryev, A.D Institute of Cytology of Russian Academy of Sciences, St. Petersburg, Russia , Glushankova, L.N Institute of Cytology of Russian Academy of Sciences, St. Petersburg, Russia , Shalygin, A.V Institute of Cytology of Russian Academy of Sciences, St. Petersburg, Russia , Wang, G College of Pharmaceutical Sciences - Soochow University, Suzhou, Jiangsu, China , Kartzev, V.G InterBioscreen Ltd., Chernogolovka, Russia , Kaznacheyeva, E.V Institute of Cytology of Russian Academy of Sciences, St. Petersburg, Russia
Pages
7
From page
140
To page
146
Abstract
Store-operated 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 μM) and had almost no effect on the STIM1-dependent activation of store-operated channels.
Keywords
Orai , 2-APB , STIM2 , STIM1 , store-operated Ca2+ entry , calcium
Journal title
Acta Naturae
Serial Year
2021
Record number
2617419
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