Store-operated CRAC channel inhibitors: opportunities and challenges

摘要

Aberrant Ca²⁺ release-activated Ca²⁺ (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 Ca²⁺ channel in different types of cells.