Target intelligence / Profile preview

Orai1-containing CRAC Channel (CRAC Channel (Orai1))

Target: CRAC Channel (Orai1)
Molecular classification: Ion channel, Calcium channel

Overview

The Orai1-containing CRAC (Calcium Release-Activated Calcium) channel is a highly Ca²⁺-selective ion channel in the plasma membrane of non-excitable cells. It is essential for store-operated calcium entry (SOCE), replenishing intracellular calcium stores and regulating numerous cellular functions, including gene expression, motility, proliferation, and immune responses. The functional channel is a hexamer of Orai1 subunits, activated by STIM1 upon ER calcium store depletion. It is a therapeutic target for autoimmune diseases and inflammatory conditions.

Other names: Calcium Release-Activated Calcium Channel (Orai1)Orai1 ChannelStore-Operated Calcium Entry Channel (Orai1)

Mechanism of action

Inhibition or modulation of calcium influx through the CRAC channel.

Biological functions

Store-operated calcium entry (SOCE)Calcium signalingGene expression regulationImmune responseCell proliferationCell motility

Disease associations

ImmunodeficiencyAutoimmune diseasesInflammationAcute pancreatitisVascular dysfunction

Safety considerations

Potential for immunosuppressionAltered calcium signaling leading to various cellular dysfunctions

Interacting drugs

2-aminoethyldiphenyl borate (2-APB)

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