A Novel Modulator of STIM2-Dependent Store-Operated Ca2+ Channel Activity
| Autor: | Alexey Shalygin, Andrey D. Grigoryev, Anton Skopin, L. N. Glushankova, Guanghui Wang, Elena Kaznacheyeva, Viktor G. Kartzev |
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| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
STIM2 Orai STIM1 chemistry.chemical_element Calcium Biochemistry 03 medical and health sciences 0302 clinical medicine Molecular Biology IC50 store-operated Ca2+ entry calcium Chemistry Endoplasmic reticulum 2-APB Small molecule Cell biology 030104 developmental biology Molecular Medicine Ca2 channels 030217 neurology & neurosurgery Intracellular Research Article Biotechnology |
| Zdroj: | Acta Naturae |
| ISSN: | 2075-8251 |
| DOI: | 10.32607/actanaturae.11269 |
| Popis: | 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 M) and had almost no effect on the STIM1-dependent activation of store-operated channels. |
| Databáze: | OpenAIRE |
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