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Structural Modelling of the Human Drug-Metabolizing Cytochromes P450

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Abstract:

The structural and functional aspects of cytochrome P450 (CYP) enzymes are reviewed in the light of current developments in X-ray crystallography and other physical evidence, together with recent findings on the regulation of, and polymorphisms in, the human drug-metabolizing CYPs. It is emphasized that the crystal structures of eukaryotic CYPs are particuarly useful for constructing homology models of the human enzymes associated with drug metabolism, and that these models can aid in the high-throughput screening of novel compounds destined for human exposure.

Keywords: Cytochromes P450 (CYPs); drug metabolism; enzyme structure and function

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986706778201567

Affiliations: School of Biomedical and Molecular Sciences, University of Surrey, Guildford, Surrey, GU2 7XH,UK.

Publication date: September 1, 2006

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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