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.
Keywords:
CRAC channel inhibitor; Ca2+ release-activated Ca2+ channel; ORAI1; STIM1; store-operated Ca2+ entry.
Publication types
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Review
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Research Support, Non-U.S. Gov't
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Calcium / metabolism
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Calcium Channel Blockers / chemistry
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Calcium Channel Blockers / pharmacology*
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Calcium Channel Blockers / therapeutic use
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Calcium Release Activated Calcium Channels / antagonists & inhibitors*
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Calcium Release Activated Calcium Channels / metabolism
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Humans
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Molecular Targeted Therapy
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ORAI1 Protein / antagonists & inhibitors
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ORAI1 Protein / metabolism
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Stromal Interaction Molecule 1 / antagonists & inhibitors
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Stromal Interaction Molecule 1 / metabolism
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Structure-Activity Relationship
Substances
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Calcium Channel Blockers
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Calcium Release Activated Calcium Channels
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ORAI1 Protein
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Stromal Interaction Molecule 1
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Calcium