Protein Information

Name CYP2B
Synonyms CYP2B; CYP2B7; CYP2B7P; CYP2B protein; CYP2B7P1; CYP2B7P1 protein; CYP2B7P1 proteins

Compound Information

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

Reference List

PubMed Abstract RScore(About this table)
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.

The evidence indicates that ring-hydroxylation is catalyzed by CYP2B: a) induction of CYP2B was required for ring-hydroxylation; b) antibodies against CYP2B1/2 strongly inhibited the formation of the ring-hydroxylated products by PB microsomes; c) incubation of methoxychlor with reconstituted CYP2B1 yielded both the hydroxylated (IV and VII) and the demethylated (II and III) metabolites; and d) reconstituted CYP2B1 converted mono-OH-M into bis-OH-M and tris-OH-M, whereas bis-OH-M was converted into tris-OH-M.
33(0,1,1,3) 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.
32(0,1,1,2) Details
9736480 Li HC, Kupfer D: Mechanism of induction of rat hepatic CYP2B and 3A by the pesticide methoxychlor. J Biochem Mol Toxicol. 1998;12(6):315-23.
32(0,1,1,2) Details
12919727 Oropeza-Hernandez LF, Lopez-Romero R, Albores A: Hepatic CYP1A, 2B, 2C, 2E and 3A regulation by methoxychlor in male and female rats. Toxicol Lett. 2003 Sep 15;144(1):93-103.

On the contrary, females were more responsive than males for pentoxyresorufin-O-dealkylase (PROD) and benzyloxyresorufin-O-dearylase (BROD), two CYP2B-related activities.
1(0,0,0,1) Details
9241656 Ekins S, VandenBranden M, Ring BJ, Wrighton SA: Examination of purported probes of human CYP2B6. . Pharmacogenetics. 1997 Jun;7(3):165-79.

A commercially available antibody to rat CYP2B, suggested to be specific for CYP2B6, was found to cross react with all members to the CYP2 family examined including CYP2C19, which possessed a nearly identical electrophoretic mobility to that of CYP2B6 in the system examined.
Methoxychlor and S-mephenytoin inhibited expressed CYP2B6 but not CYP1A2 mediated 7-EFC O-deethylation.
1(0,0,0,1) Details
15649640 Dehn PF, Allen-Mocherie S, Karek J, Thenappan A: Organochlorine insecticides: impacts on human HepG2 cytochrome P4501A, 2B activities and glutathione levels. Toxicol In Vitro. 2005 Mar;19(2):261-73.

This study examined the effects of the organochlorine (OC) insecticides chlordane, o,p'-DDT, dieldrin, endosulfan, kepone, methoxychlor, and toxaphene on human HepG2 cytochrome P450 (1A-EROD and 2B-PROD) activities and glutathione (GSH) levels.
These results support findings of OC insecticides inducing CYP1A, 2B in rats, with CYP2B responses more important.
1(0,0,0,1) Details
16054614 Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? . Chem Biol Interact. 2005 Aug 15;155(3):111-28.

Furthermore, PXR and CAR induce enzymes, such as the CYP2B and CYP3A family members, responsible for the metabolism of steroid and thyroid hormones and this may alter their normal physiological function.
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
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.
0(0,0,0,0) Details
7595932 Li HC, Dehal SS, Kupfer D: Induction of the hepatic CYP2B and CYP3A enzymes by the proestrogenic pesticide methoxychlor and by DDT in the rat. J Biochem Toxicol. 1995 Feb;10(1):51-61.

Additional indication of methoxychlor- and DDT-mediated induction of CYP2B enzymatic activity in mature and immature rats was evident from increased ring hydroxylation of methoxychlor, an activity attributed to CYP2B.
174(2,2,4,4) Details
8789153 Stresser DM, Dehal SS, Kupfer D: Ring hydroxylation of [o-3H] methoxychlor as a probe for liver microsomal CYP2B activity: potential for in vivo CYP2B assay. Anal Biochem. 1996 Jan 1;233(1):100-7.
37(0,1,1,7) Details