Protein Information

Name CYP3A4
Synonyms CP33; CYP3; HLP; CYP3A; CP34; CYP 3A4; CYP 3; CYP3A3…

Compound Information

Name acrolein
CAS 2-propenal

Reference List

PubMed Abstract RScore(About this table)
19103281 Park D, Jeon JH, Shin S, Joo SS, Kang DH, Moon SH, Jang MJ, Cho YM, Kim JW, Ji HJ, Ahn B, Oh KW, Kim YB: Green tea extract increases cyclophosphamide-induced teratogenesis by modulating the expression of cytochrome P-450 mRNA. Reprod Toxicol. 2009 Jan;27(1):79-84. Epub 2008 Dec 3.

Moreover, repeated treatment with GTE greatly increased mRNA expression and activity of hepatic cytochrome P-450 (CYP) 2B, which metabolizes cyclophosphamide into teratogenic acrolein and cytotoxic phosphoramide mustard, while reducing CYP3A expression (a detoxifying enzyme).
82(1,1,1,2) Details
9622079 Egorin MJ, Rosen DM, Wolff JH, Callery PS, Musser SM, Eiseman JL: Metabolism of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) by murine and human hepatic preparations. Cancer Res. 1998 Jun 1;58(11):2385-96.

Incubation of 17AAG with cloned CYP3A4 produced metabolites 4 and 6.
These data have implications with regard to preclinical toxicology and activity testing of 17AAG as well as its proposed clinical development because: (a) production of 17AG requires concomitant production of acrolein from the cleaved allyl moiety; and (b) 17AG, which was not metabolized by microsomes, has been described as being as active as 17AAG in decreasing cellular p185erbB2.
2(0,0,0,2) Details
19017849 Storme T, Deroussent A, Mercier L, Prost E, Re M, Munier F, Martens T, Bourget P, Vassal G, Royer J, Paci A: New ifosfamide analogs designed for lower associated neurotoxicity and nephrotoxicity with modified alkylating kinetics leading to enhanced in vitro anticancer activity. J Pharmacol Exp Ther. 2009 Feb;328(2):598-609. Epub 2008 Nov 18.

Isophosphoramide mustard is the bisalkylating active metabolite, and acrolein is a urotoxic side product.
Metabolite determinations of the dimethyl-ifosfamide analogs were performed using liquid chromatography and tandem mass spectrometry after in vitro biotransformation by drug-induced rat liver microsomes and human microsomes expressing the main CYP3A4 and minor CYP2B6 enzymes.
1(0,0,0,1) Details