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Overview
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Background
CITCO, an imidazothiazole derivative, is a selective agonist of human CAR, with an EC50 value of 49 nM and > 50-fold selectivity to CAR over pregnane X receptor (PXR), and no activity on other nuclear receptors. Upon activation with specific agonists, CAR translocates into the nucleus and binds to the response elements as monomers or CAR/RXR heterodimers. The CAR functions as a xenobiotic receptor, involved in detoxification and clearance of toxic substances from the liver. In addition, activation with selective CAR agonists such as CITCO has also been shown to inhibit growth and expansion of brain tumor stem cells.
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