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Literature DB >> 27149324

Store-operated CRAC channel inhibitors: opportunities and challenges.

Chengsen Tian¹, Lupei Du¹, Yubin Zhou², Minyong Li¹.

Abstract

Aberrant Ca(2+) release-activated Ca(2+) (CRAC) channel activity has been implicated in a number of human disorders, including immunodeficiency, autoimmunity, occlusive vascular diseases and cancer, thus placing CRAC channels among the important targets for the treatment of these disorders. We briefly summarize herein the molecular basis and activation mechanism of CRAC channel and focus on discussing several pharmacological inhibitors of CRAC channels with respect to their biological activity, mechanisms of action and selectivity over other types of Ca(2+) channel in different types of cells.

Entities: Chemical Disease Species

Keywords: CRAC channel inhibitor; Ca2+ release-activated Ca2+ channel; ORAI1; STIM1; store-operated Ca2+ entry

Mesh：

Substances：

Year: 2016 PMID： 27149324 PMCID： PMC5558521 DOI： 10.4155/fmc-2016-0024

Source DB: PubMed Journal: Future Med Chem ISSN： 1756-8919 Impact factor: 3.808

132 in total

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