CAR Activity

Although PB treatment induces the nuclear translocation and transcriptional activity of CAR, results from ligand-binding assays have indicated that neither PB nor known PB metabolites are 

Ligands that bind directly to CAR have also been identified. Initially, in a search for CAR activators, it was discovered that the constitutive activity of CAR could be repressed by androstanes, which are testosterone metabolites . As a result, CAR is now known as the constitutive androstane receptor. Androstanes bind CAR directly to repress its transcriptional activity and have been termed inverse agonists While 

Direct-binding xenobiotic ligands of CAR have also been identified and many of these show marked species specificity as well. For example, the planar hydrocarbon l,4-bis[2-(3,5-dichloropy-ridyloxy)]benzene binds directly to mCAR and is 

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Disorders with enhanced sensitivity of the CaR to CaQ+. In contrast to inactivating mutations of the CaR, activating antibodies produce a syndrome of autosomal... 

CAR activators in humans—3-MC, phenylpropionic acid, phenobarbital, phenytoin, carbamazepine. 

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Prior to the publication of the first X-ray structures of CAR [185,186,187] some pharmacophore models had been generated. Based on small numbers of molecules suggested to be mouse CAR activators, a study of Ekins et al. 

Table 17.5 summarizes the specificity and WOE of the PPARa activator MOA. The WOE strongly supports the MOA due to the large number of smdies that have been carried out since the discovery of peroxisome proliferation by these chemicals in 1965 (Hess et al. 1965). PPARa activation is by definition specific, because this key event is distinct from other initiating events such as CAR activation or increases in cytotoxicity. The other key events by themselves are considered to... 

The number of PXR and CAR activators will continue to increase and the identification of more endogenous as well as environmental chemicals that modulate the xenobiotic receptors will improve our understanding of the mechanisms by which environmental compounds affect our endocrine balance and may offer novel strategies for preventing chemical toxicity. 

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