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Whole-Cell Recording of Calcium Release-Activated Calcium CRAC Currents in Human T Lymphocytes
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Store-operated CRAC channel inhibitors: opportunities and challenges

Chengsen Tian1, Lupei Du1, Yubin Zhou2

  • 1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.

Future Medicinal Chemistry
|May 6, 2016
PubMed

Insights

Aberrant calcium release-activated calcium (CRAC) channel activity is linked to diseases like cancer and immunodeficiency. This review covers CRAC channel mechanisms and highlights key pharmacological inhibitors for therapeutic development.

Area of Science:

  • Biochemistry and Molecular Biology
  • Pharmacology
  • Cell Physiology

Background:

  • Aberrant calcium release-activated calcium (CRAC) channel activity is associated with various human diseases, including immunodeficiency, autoimmunity, vascular diseases, and cancer.
  • CRAC channels are crucial for cellular calcium homeostasis and signaling pathways.
  • These channels represent significant therapeutic targets for managing these disorders.

Purpose of the Study:

  • To summarize the molecular basis and activation mechanisms of CRAC channels.
  • To discuss various pharmacological inhibitors of CRAC channels.
  • To evaluate the biological activity, mechanisms of action, and selectivity of these inhibitors.

Main Methods:

  • Literature review of CRAC channel research.
  • Analysis of published data on CRAC channel inhibitors.
  • Comparative evaluation of inhibitor properties.

Main Results:

  • Detailed overview of CRAC channel structure and function.
  • Identification and characterization of several CRAC channel inhibitors.
  • Assessment of inhibitor selectivity across different cell types and calcium channels.

Conclusions:

  • CRAC channels are validated drug targets for multiple diseases.
  • Pharmacological inhibition of CRAC channels shows therapeutic potential.
  • Further research into selective CRAC inhibitors is warranted for clinical applications.
Keywords:
CRAC channel inhibitorCa2+ release-activated Ca2+ channelORAI1STIM1store-operated Ca2+ entry

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