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...

Descripción completa

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
_version_ 1783686128140812288
author Skopin, A. Y.
Grigoryev, A. D.
Glushankova, L. N.
Shalygin, A. V.
Wang, G.
Kartzev, V. G.
Kaznacheyeva, E. V.
author_facet Skopin, A. Y.
Grigoryev, A. D.
Glushankova, L. N.
Shalygin, A. V.
Wang, G.
Kartzev, V. G.
Kaznacheyeva, E. V.
author_sort Skopin, A. Y.
collection PubMed
description 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.
format Online
Article
Text
id pubmed-8084296
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher A.I. Gordeyev
record_format MEDLINE/PubMed
spelling pubmed-80842962021-05-05 A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity Skopin, A. Y. Grigoryev, A. D. Glushankova, L. N. Shalygin, A. V. Wang, G. Kartzev, V. G. Kaznacheyeva, E. V. Acta Naturae Research Article 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. A.I. Gordeyev 2021 /pmc/articles/PMC8084296/ /pubmed/33959394 http://dx.doi.org/10.32607/actanaturae.11269 Text en Copyright ® 2021 National Research University Higher School of Economics. https://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Skopin, A. Y.
Grigoryev, A. D.
Glushankova, L. N.
Shalygin, A. V.
Wang, G.
Kartzev, V. G.
Kaznacheyeva, E. V.
A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
title A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
title_full A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
title_fullStr A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
title_full_unstemmed A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
title_short A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
title_sort novel modulator of stim2-dependent store-operated ca2+ channel activity
topic Research Article
url 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
work_keys_str_mv AT skopinay anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT grigoryevad anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT glushankovaln anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT shalyginav anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT wangg anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT kartzevvg anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT kaznacheyevaev anovelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT skopinay novelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT grigoryevad novelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT glushankovaln novelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT shalyginav novelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT wangg novelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT kartzevvg novelmodulatorofstim2dependentstoreoperatedca2channelactivity
AT kaznacheyevaev novelmodulatorofstim2dependentstoreoperatedca2channelactivity

Ejemplares similares