Protein Information

Name cytochrome P450 3A4
Synonyms CP33; CYP3; HLP; CYP3A; CP34; CYP 3A4; CYP 3; CYP3A3…

Compound Information

Name endosulfan
CAS 6,7,8,9,10,10-hexachloro-1,5,5a,6,9,9a-hexahydro-6,9-methano-2,4,3-benzodioxathiepin 3-oxide

Reference List

PubMed Abstract RScore(About this table)
16855053 Casabar RC, Wallace AD, Hodgson E, Rose RL: Metabolism of endosulfan-alpha by human liver microsomes and its utility as a simultaneous in vitro probe for CYP2B6 and CYP3A4. Drug Metab Dispos. 2006 Oct;34(10):1779-85. Epub 2006 Jul 19.
100(0,3,4,5) Details
17936932 Hodgson E, Rose RL: Human metabolic interactions of environmental chemicals. J Biochem Mol Toxicol. 2007;21(4):182-6.

Endosulfan-alpha, which has shown promise as a model substrate for phenotyping CYP3A4 and CYP2B6 in human liver microsomes, is also an inducer of CYP2B6, acting through the PXR receptor.
82(1,1,1,2) Details
16581944 Lee HK, Moon JK, Chang CH, Choi H, Park HW, Park BS, Lee HS, Hwang EC, Lee YD, Liu KH, Kim JH: Stereoselective metabolism of endosulfan by human liver microsomes and human cytochrome P450 isoforms. Drug Metab Dispos. 2006 Jul;34(7):1090-5. Epub 2006 Mar 31.

The P450 isoform-selective inhibition study in human liver microsomes and the incubation study of cDNA-expressed enzymes also demonstrated that the stereoselective sulfonation of alpha-endosulfan is mediated by CYP2B6, CYP3A4, and CYP3A5, and that that of beta-endosulfan is transformed by CYP3A4 and CYP3A5.
199(2,3,4,4) 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