A new selective pharmacological enhancer of the Orai1 Ca2+ channel reveals roles for Orai1 in smooth and skeletal muscle functions.

ABSTRACT: Store operated calcium (Ca2+) entry is an important homeostatic mechanism in cells, whereby the release of Ca2+ from intracellular endoplasmic reticulum stores triggers the activation of a Ca2+ influx pathway. Mediated by Orai1, this Ca2+ influx has specific and essential roles in biological processes as diverse as lactation to immunity. Although pharmacological inhibitors of this Ca2+ influx mechanism have helped to define the role of store operated Ca2+ entry in many cellular events, the lack of isoform specific modulators and activators of Orai1 has limited our full understanding of these processes. Here we report the identification and synthesis of an Orai1 activity enhancer that concurrently potentiated Orai1 Ca2+ -dependent inactivation (CDI). This unique enhancer of Orai1 had only a

SUBMITTER: Azimi I 

PROVIDER: S-EPMC7079732 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature