Cytochrome P450: Role in the Metabolism and Toxicity of by Costas Ioannides, Diana Anderson, Xinxin Ding, Graeme

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

This a lot wanted, new, absolutely up to date book fills this hole and emphasizes the hot correct subject matters that experience emerged over the last decade in an simply obtainable demeanour. The enzyme method, cytochromes P450, contains a few families/subfamilies, and the focal point of the e-book is to house every one separately, furnishing info at once correct to scientists taken with the advance of chemical compounds, specifically within the evaluate in their safeguard. The publication has contributions from across the world revered scientists who're research-active within the appropriate components. The authors have made vast use of figures and tables in order that the reader can entry the required info with no consistently having to learn the textual content. additionally, a truly vast, uncomplicated index is a different hallmark of the publication. 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 offers with the function of this enzyme within the formation of reactive intermediates. The smart and large usage of the molecular biology method very speedily resulted in an enormous 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 means of the 10 chapters partly B of this booklet, facing ten subfamilies and households of cytochrome P450. half C deals an perception into one other element of cytochrome P450 learn, particularly its legislation via receptor-mediated stimuli - rather than enzyme induction or inhibition. the ultimate bankruptcy interprets the present facts on one of the drug metabolizing platforms into medical software and highlights the position of cytochromes P450 within the therapy of neoplastic development. The ebook offers generally with every one family/subfamily of the cytochromes P450 that give a contribution to the metabolism of xenobiotics.

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

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The Fe–S bond length changes during the course of the catalytic cycle, this being dependent upon the redox and spin-states of the iron atom. 3. In general, the change from lowspin (LS) to high-spin (HS) increases the Fe–S distance slightly, and Fe(III) generally shows a shorter Fe–S bond than for Fe(II). 4. The effect of the changes in iron spin-state on the haem geometry usually involves a movement of the iron atom out of the porphyrin ring plane and towards the cysteine sulphur when iron is in the high-spin state due to its increased ionic radius.

9 provides a listing of selective human P450 substrates for the major drug-metabolising P450s. The substrate selectivities for the eight human P450s which comprise the major drug-metabolising enzymes appear to be largely determined by compound molecular size (Mr), acid/base characteristics (pKa) and the ability to form hydrogen bonds with the enzyme, which relates to the number of hydrogen bond acceptors and donors in the molecule (NA+D HB ). 9 Chapter 1 Selective human CYP substrates. CYP1A2 Antipyrine Caffeine Clozapine Clomipramine Imipramine Paracetamol (acetaminophen) Phenacetin Propranolol Tacrine Theophylline CYP2A6 Coumarin Nicotine Cotinine Fadrozole SM-12502 Losigamone 4-Nitroanisole 2,6-Dichlorobenzonitrile Quinoline Indole CYP2B6 7-Benzyloxyresorufin 7-Ethoxy-4-trifluoromethylcoumarin Deprenyl Testosterone Benzphetamine Bupropion PNU 249173 Cinnarizine 7-Ethoxycoumarin Arteether CYP2C9 Antipyrine Diclofenac Phenytoin S-Warfarin Tolbutamide R-Naproxen 86,153 Tienilic acid Ibuprofen Flurbiprofen Mefenamic acid CYP2C19 Amitriptyline Citalopram Clomipramine Diazepam Imipramine Mephobarbital Omeprazole Proguanil Propranolol S-Mephenytoin CYP2D6 Aprindine Encainide Mexiletine Propafenone Metoprolol Propranolol Perphenazine Haloperidol Thioridazine Zuclopenthixol Codeine Dextromethorphan Dihydrocodeine Ethylmorphine Hydrocodone Tramadol Fluoxetine Paroxetine Amitriptyline Clomipramine Desipramine Imipramine N-Desmethylclomipramine Nortriptyline Trimipramine Maprotiline MDMA Debrisoquine Sparteine CYP2E1 Chlorzoxazone Enflurane Halothane Paracetamol (acetaminophen) Salicylic acid Benzene Ethanol Dimethylnitrosamine 4-Nitrophenol Dapsone CYP3A4 Amiodarone Lidocaine Propafenone Quinidine Ifosfamide Tamoxifen Toremifene Vinblastine Alprazolam Diazepam Midazolam Triazolam Diltiazem Felopidine Nifedipine Verapamil Cortisol Ethynyloestradiol Testosterone Carbamazepine Clomipramine Cyclosporin A Erythromycin Imipramine Omeprazole Proguanil Terfenadine remaining compound set.

In general, the change from lowspin (LS) to high-spin (HS) increases the Fe–S distance slightly, and Fe(III) generally shows a shorter Fe–S bond than for Fe(II). 4. The effect of the changes in iron spin-state on the haem geometry usually involves a movement of the iron atom out of the porphyrin ring plane and towards the cysteine sulphur when iron is in the high-spin state due to its increased ionic radius. 5. 05A˚ with only slight variations between different P450s and within the reaction cycle itself.

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