The use of the substrate-heme complex approach in the design, synthesis, biochemical evaluation, and rationalization of the inhibitory activity of a range of azole compounds against cholesterol side chain cleavage enzyme

Ahmed, Sabbir (2000) The use of the substrate-heme complex approach in the design, synthesis, biochemical evaluation, and rationalization of the inhibitory activity of a range of azole compounds against cholesterol side chain cleavage enzyme. Biochemical and Biophysical Research Communications, 275(1), pp. 75-76. ISSN (print) 0006-291X

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Abstract

Here, we report the synthesis and biochemical evaluation of a number of compounds as potent inhibitors of cytochrome P450 enzymes, such as aromatase (AR), but not cholesterol side chain cleavage (CSCC). This is a crucial enzyme in the steroidal cascade and its inhibition results in major side-effects, as a result, the ability of compounds to specifically inhibit enzymes such as AR but not CSCC would be an important factor in the drug design process.

Item Type: Article
Uncontrolled Keywords: molecular modeling perspective, aromatase, mechanism
Research Area: Chemistry
Faculty, School or Research Centre: Faculty of Science (until 2011) > School of Pharmacy and Chemistry
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Depositing User: Automatic Import Agent
Date Deposited: 16 Mar 2010 08:08
Last Modified: 08 Apr 2011 11:19
URI: http://eprints.kingston.ac.uk/id/eprint/7241

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