P450 (cytochrome P450) enzymes have major roles in the biosynthesis of endogenous factors such as steroids and eicosanoids, in the termination of the action of endogenous factors such as retinoic acid, in the metabolism of most drugs and xenobiotics and in the generation of toxic and carcinogenic products. Understanding the determinants of the substrate and inhibitor specificities of these enzymes is important for drug design. The crystallographic analysis of the deformability of two bacterial P450 active sites associated with the binding of azole (a class of inhibitors with an imidazole or triazole ring that co-ordinates to the haem iron) inhibitors described in the present study illustrates the importance of protein conformational malleability in the binding of imidazole derivatives.
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December 2006
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Conference Article|
October 25 2006
Protein dynamics and imidazole binding in cytochrome P450 enzymes
A. Verras;
A. Verras
1Department of Pharmaceutical Chemistry, University of California, 600, 16th Street, San Francisco, CA 94143-228, U.S.A.
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P.R. Ortiz de Montellano
P.R. Ortiz de Montellano
1
1Department of Pharmaceutical Chemistry, University of California, 600, 16th Street, San Francisco, CA 94143-228, U.S.A.
1To whom correspondence should be addressed, at the University of California, Genentech Hall GH-N572D, 600, 16th Street, San Francisco, CA 94143-2280, U.S.A. (email ortiz@cgl.ucsf.edu).
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Publisher: Portland Press Ltd
Received:
June 21 2006
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2006 The Biochemical Society
2006
Biochem Soc Trans (2006) 34 (6): 1170–1172.
Article history
Received:
June 21 2006
Citation
A. Verras, P.R. Ortiz de Montellano; Protein dynamics and imidazole binding in cytochrome P450 enzymes. Biochem Soc Trans 1 December 2006; 34 (6): 1170–1172. doi: https://doi.org/10.1042/BST0341170
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