Protein Information

Name CYP2B6
Synonyms CPB 6; CPB6; CYP2B; CYP2B protein; CYP2B6; CYPIIB 6; CYPIIB6; Cytochrome P450 2B6…

Compound Information

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

Reference List

PubMed Abstract RScore(About this table)
10101147 Stresser DM, Kupfer D: Monospecific antipeptide antibody to cytochrome P-450 2B6. Drug Metab Dispos. 1999 Apr;27(4):517-25.

The utility of this antibody for determining human liver microsomal CYP2B6 contribution to the ortho-hydroxylation of methoxychlor was demonstrated.
88(1,1,1,8) Details
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.

Methoxychlor, a structural analog of the DDT pesticide, was previously shown to induce rat hepatic CYP2B and -3A mRNAs and the corresponding proteins [J Biochem Mol Toxicol 1998;12:315-323], Additionally, methoxychlor was found to activate the constitutive androstane receptor (CAR) system and induce CYP2B6 (J Biol Chem 1999;274:6043-6046), suggesting a mechanism for methoxychlor-mediated cytochrome P450 (P450) 2B induction.
81(1,1,1,1) Details
9241656 Ekins S, VandenBranden M, Ring BJ, Wrighton SA: Examination of purported probes of human CYP2B6. . Pharmacogenetics. 1997 Jun;7(3):165-79.

Methoxychlor and S-mephenytoin inhibited expressed CYP2B6 but not CYP1A2 mediated 7-EFC O-deethylation.
6(0,0,0,6) Details
9733665 Stresser DM, Kupfer D: Human cytochrome P450-catalyzed conversion of the proestrogenic pesticide methoxychlor into an estrogen. Drug Metab Dispos. 1998 Sep;26(9):868-74.

CYP2B6 and CYP2C9 were much less active.
2(0,0,0,2) Details
12167570 Hu Y, Kupfer D: Metabolism of the endocrine disruptor pesticide-methoxychlor by human P450s: pathways involving a novel catechol metabolite. Drug Metab Dispos. 2002 Sep;30(9):1035-42.

CYP2B6 appeared unique, catalyzing effectively both O-demethylation and ortho-hydroxylation.
1(0,0,0,1) Details
9047321 Stresser DM, Kupfer D: Catalytic characteristics of CYP3A4: requirement for a phenolic function in ortho hydroxylation of estradiol and mono-O-demethylated methoxychlor. Biochemistry. 1997 Feb 25;36(8):2203-10.

0(0,0,0,0) Details
7895613 Dehal SS, Kupfer D: Metabolism of the proestrogenic pesticide methoxychlor by hepatic P450 monooxygenases in rats and humans. Drug Metab Dispos. 1994 Nov-Dec;22(6):937-46.

Human CYP2B6 exhibits ring-hydroxylation, indicating that this reaction is catalyzed by several CYP2B isozymes.
1(0,0,0,1) Details