Protein Information

Name constitutive androstane receptor
Synonyms CAR; CAR beta; CAR 1; CAR1; CARb; CARbeta; Constitutive activator of retinoid response; Constitutive active response…

Compound Information

Name methoxychlor
CAS 1,1′-(2,2,2-trichloroethylidene)bis[4-methoxybenzene]

Reference List

PubMed Abstract RScore(About this table)
11353743 Blizard D, Sueyoshi T, Negishi M, Dehal SS, Kupfer D: Mechanism of induction of cytochrome p450 enzymes by the proestrogenic endocrine disruptor pesticide-methoxychlor: interactions of methoxychlor metabolites with the constitutive androstane receptor system. Drug Metab Dispos. 2001 Jun;29(6):781-5.
162(2,2,2,2) Details
18973326 Repo S, Jyrkkarinne J, Pulkkinen JT, Laatikainen R, Honkakoski P, Johnson MS: Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. J Med Chem. 2008 Nov 27;51(22):7119-31.

2(0,0,0,2) Details
12948398 Makinen J, Reinisalo M, Niemi K, Viitala P, Jyrkkarinne J, Chung H, Pelkonen O, Honkakoski P: Dual action of oestrogens on the mouse constitutive androstane receptor. . Biochem J. 2003 Dec 1;376(Pt 2):465-72.

This novel dual action is not limited to oestrogens, but is shared by some xenobiotic CYP2B inducers such as clotrimazole and methoxychlor.
2(0,0,0,2) Details
16054614 Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? . Chem Biol Interact. 2005 Aug 15;155(3):111-28.

The pregnane X-receptor (PXR) and the constitutive androstane receptor (CAR) are orphan nuclear receptors activated by a variety of ligands.
Environmental estrogens, such as the pesticides methoxychlor, endosulfan, dieldrin, DDT, and the plasticizer nonylphenol activate either PXR or both PXR and CAR.
1(0,0,0,1) Details
15466163 Yueh MF, Kawahara M, Raucy J: High volume bioassays to assess CYP3A4-mediated drug interactions: induction and inhibition in a single cell line. Drug Metab Dispos. 2005 Jan;33(1):38-48. Epub 2004 Oct 1.

Treatment of stable transformants, namely DPX-2, with various concentrations of inducers including rifampicin, mifepristone, troglitazone, methoxychlor, and kava produced dose-dependent increases in luciferase expression (between 2- and 40-fold above dimethyl sulfoxide-treated cells).
Constitutive androstane receptor-mediated regulation of CYP3A4 protein was addressed by measuring catalytic activity in a separate cell line over-expressing this receptor.
1(0,0,0,1) Details