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

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 p...

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Detalles Bibliográficos
Autores principales: Skopin, A. Y., Grigoryev, A. D., Glushankova, L. N., Shalygin, A. V., Wang, G., Kartzev, V. G., Kaznacheyeva, E. V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: A.I. Gordeyev 2021
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8084296/
https://www.ncbi.nlm.nih.gov/pubmed/33959394
http://dx.doi.org/10.32607/actanaturae.11269
Descripción
Sumario: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 (IC50 = 1 μM) and had almost no effect on the STIM1-dependent activation of store-operated channels.

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