Store-operated CRAC channel inhibitors: opportunities and challenges. Academic Article

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

• Zhou, Yubin

published proceedings

• Future Med Chem

author list (cited authors)

• Tian, C., Du, L., Zhou, Y., & Li, M.

citation count

• 69

complete list of authors

• Tian, Chengsen||Du, Lupei||Zhou, Yubin||Li, Minyong

publication date

• May 2016

publisher

• Future Science Ltd  Publisher

published in

• Future Medicinal Chemistry  Journal

keywords

• Animals
• Ca2+ Release-activated Ca2+ Channel
• Calcium
• Calcium Channel Blockers
• Calcium Release Activated Calcium Channels
• Crac Channel Inhibitor
• Humans
• Molecular Targeted Therapy
• ORAI1 Protein
• Orai1
• STIM1
• Store-operated Ca2+ Entry
• Stromal Interaction Molecule 1
• Structure-Activity Relationship

PubMed Central ID

• 27149324

Digital Object Identifier (DOI)

• 10.4155/fmc-2016-0024

start page

• 817

end page

• 832

volume

• 8

issue

• 7