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Inhibitors of cytochrome P450 (CYP) 1B1.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2017 Jul 28; Vol. 135, pp. 296-306. Date of Electronic Publication: 2017 Apr 18. - Publication Year :
- 2017
-
Abstract
- Human cytochrome P450 1B1 (CYP1B1) is involved in the metabolism of various drugs. This enzyme catalyzes the hydroxylation of aryl compounds, thus generating more polar metabolites that can be easily excreted. CYP1B1 is also known for its ability to activate procarcinogens into carcinogens. For example, it can hydroxylate 17β-estradiol (E2) into 4-hydroxy-E2, which can promote tumorigenesis as a potent estrogen, or after being transformed into E2-3,4-quinone. Since elevated expression levels of CYP1B1 have been reported in various cancers, but not in normal tissues, this enzyme represents an interesting therapeutic target. This review put emphasis on different families of inhibitors, especially those reported since 2003.<br /> (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 135
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 28458135
- Full Text :
- https://doi.org/10.1016/j.ejmech.2017.04.042