By Costas Ioannides, Diana Anderson, Xinxin Ding, Graeme Murray, David Lewis, Olavi Pelkonen, Stephen S Ferguson, A E Rettie, K H Chang, M Negishi, Raymond F Novak, Morag HcFaoyen, Yuko Ito, B Moorthy, Hermann M Bolt, M Murray, D J Greenblatt, P H Roos, Lau

ISBN-10: 0854042741

ISBN-13: 9780854042746

This a lot wanted, new, absolutely up to date book fills this hole and emphasizes the hot correct themes that experience emerged over the past decade in an simply obtainable demeanour. The enzyme approach, cytochromes P450, includes a few families/subfamilies, and the point of interest of the e-book is to accommodate every one separately, furnishing info at once correct to scientists all for the improvement of chemical substances, specifically within the review in their defense. The e-book has contributions from the world over revered scientists who're research-active within the suitable parts. The authors have made huge use of figures and tables in order that the reader can entry the required info with out consistently having to learn the textual content. furthermore, a truly wide, easy index is a special hallmark of the ebook. half A of this monograph introduces the reader to the present wisdom of the evolutionary improvement of cytochrome P450 constitution and serve as. moreover, it bargains with the position of this enzyme within the formation of reactive intermediates. The clever and vast usage of the molecular biology technique very quickly ended in an unlimited physique of enzymes calling for a type of the plethora of alternative cytochromes P450 (the superfamily) into households and subfamilies. this is often aptly exemplified by way of the 10 chapters partly B of this ebook, facing ten subfamilies and households of cytochrome P450. half C bargains an perception into one other element of cytochrome P450 learn, specifically its rules via receptor-mediated stimuli - in preference to enzyme induction or inhibition. the ultimate bankruptcy interprets the present info on among the drug metabolizing platforms into medical software and highlights the position of cytochromes P450 within the therapy of neoplastic development. The booklet offers generally with each one family/subfamily of the cytochromes P450 that give a contribution to the metabolism of xenobiotics.

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Extra resources for Cytochrome P450: Role in the Metabolism and Toxicity of Drugs and other Xenobiotics (Issues in Toxicology)

Example text

Homology modelling from P450 crystal structures, both bacterial and mammalian, has facilitated significant exploration of the molecular determinants for substrate selectivity, and has also enabled further insights into the recognition process for substrates and their orientation for metabolism by complementary active site amino acid residues. It is clear that certain key active site residues play important roles in the molecular recognition process and, in some cases, modulate the catalytic functionalities of P450 enzymes.

Interaction with substrates in the active site region, and this is confirmed by molecular modelling studies based on the CYP2B4 crystal structure. Similar findings have been observed for other P450s, although there are often outliers and/or secondary parallel lines for different substrates which suggest that additional active site interactions are present, since the difference in intercepts indicates either an extra hydrogen bond (À2 kcal molÀ1) or a p-p stacking (À1 kcal molÀ1) interaction being formed between substrate and the enzyme’s active site region.

338 Comments Refined crystal structure Model constructed from CYP2B4a Refined crystal structure Refined crystal structure Model constructed from CYP2C9b Refined crystal structure Refined crystal structure Model constructed from CYP3A4c a ¼ 4-Chlorophenylimidazole-bound structure (pdb code: 1suo). ¼ Warfarin-bound structure (pdb code: 1og5). ¼ Metyrapone-bound structure (pdb code: 1wof). Notes: 1. In general, the substrate template size is within the volume limitations of the active site. In the case of CYP2C9, however, there is a very tight overlay of substrates which are highly superimposable, thus leading to a significantly lower volume than that available in the haem environment.

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Cytochrome P450: Role in the Metabolism and Toxicity of Drugs and other Xenobiotics (Issues in Toxicology) by Costas Ioannides, Diana Anderson, Xinxin Ding, Graeme Murray, David Lewis, Olavi Pelkonen, Stephen S Ferguson, A E Rettie, K H Chang, M Negishi, Raymond F Novak, Morag HcFaoyen, Yuko Ito, B Moorthy, Hermann M Bolt, M Murray, D J Greenblatt, P H Roos, Lau


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