title: Store-operated CRAC channel inhibitors: opportunities and challenges.
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.
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Chengsen
authors.initials: C
authors.lastname: Tian
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Lupei
authors.initials: L
authors.lastname: Du
authors.affiliation: Center for Translational Cancer Research, Institute of Biosciences & Technology, Texas A&M University Health Science Center, Houston, TX 77030, USA.
authors.forename: Yubin
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Minyong
authors.initials: M
authors.lastname: Li
mesh_terms: D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000071739:Calcium Release Activated Calcium Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D058990:Molecular Targeted Therapy; D000071740:ORAI1 Protein / Q000037:antagonists & inhibitors / Q000378:metabolism; D000071737:Stromal Interaction Molecule 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D002121:Calcium Channel Blockers; D000071739:Calcium Release Activated Calcium Channels; D000071740:ORAI1 Protein; D000071737:Stromal Interaction Molecule 1; D002118:Calcium
keywords: CRAC channel inhibitor; Ca2+ release-activated Ca2+ channel; ORAI1; STIM1; store-operated Ca2+ entry