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Curr Opin Pharmacol. 2012 Dec;12(6):696-703. doi: 10.1016/j.coph.2012.07.007. Epub 2012 Aug 21.

Cholesterol epoxide hydrolase and cancer.

Author information

1
Cancer Research Center of Toulouse, UMR 1037 INSERM-University Toulouse III, Institut Claudius Regaud, Toulouse, France. poirot.sandrine@hotmail.fr

Abstract

Cholesterol epoxide hydrolase (ChEH) catalyzes the hydration of cholesterol-5,6-epoxides (5,6-EC) into cholestane-3β,5α,6β-triol. ChEH is a hetero-oligomeric complex called the anti-estrogen binding site (AEBS) comprising 3β-hydroxysterol-Δ(8)-Δ(7)-isomerase (D8D7I) and 3β-hydroxysterol-Δ(7)-reductase (DHCR7). D8D7I and DHCR7 regulate cholesterol biosynthesis, fetal development and growth, tumor cell differentiation and death. The un-reactivity of 5,6-EC toward nucleophiles has recently been demonstrated indicating that 5,6-EC are not alkylating and carcinogenic agents as first postulated. Here we discuss recent advances in the molecular characterization of ChEH, its potential role in cancer progression and resistance as well as the interest of inhibiting ChEH and to accumulate 5,6-EC which may contribute to the anti-tumor and chemopreventive action of ChEH inhibitors used in the clinic such as tamoxifen.

PMID:
22917620
DOI:
10.1016/j.coph.2012.07.007
[Indexed for MEDLINE]

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