Journal ArticleDOI
Summary of information on human cyp enzymes: human p450 metabolism data
TLDR
This chapter is an update of the data on substrates, reactions, inducers, and inhibitors of human CYP enzymes published previously by Rendic and DiCarlo, now covering selection of the literature through 2001 in the reference section.Abstract:
This chapter is an update of the data on substrates, reactions, inducers, and inhibitors of human CYP enzymes published previously by Rendic and DiCarlo (1), now covering selection of the literature through 2001 in the reference section. The data are presented in a tabular form (Table 1) to provide a framework for predicting and interpreting the new P450 metabolic data. The data are formatted in an Excel format as most suitable for off-line searching and management of the Web-database. The data are presented as stated by the author(s) and in the case when several references are cited the data are presented according to the latest published information. The searchable database is available either as an Excel file (for information contact the author), or as a Web-searchable database (Human P450 Metabolism Database, www.gentest.com) enabling the readers easy and quick approach to the latest updates on human CYP metabolic reactions.read more
Citations
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Journal ArticleDOI
QSAR Modeling: Where have you been? Where are you going to?
Artem Cherkasov,Eugene N. Muratov,Eugene N. Muratov,Denis Fourches,Alexandre Varnek,Igor I. Baskin,Mark T. D. Cronin,John C. Dearden,Paola Gramatica,Yvonne C. Martin,Roberto Todeschini,Viviana Consonni,Victor E. Kuz’min,Richard D. Cramer,Romualdo Benigni,Chihae Yang,James F. Rathman,Lothar Terfloth,Johann Gasteiger,Ann M. Richard,Alexander Tropsha +20 more
TL;DR: In this paper, the authors provide guidelines for QSAR development, validation, and application, which are summarized in best practices for building rigorously validated and externally predictive quantitative structure-activity relationship models.
Journal ArticleDOI
Genetic polymorphisms of cytochrome P450 2D6 (CYP2D6): clinical consequences, evolutionary aspects and functional diversity
TL;DR: Predictive CYP2D6 genotyping is estimated by the author to be beneficial for treatment of about 30–40% of CYP 2D6 drug substrates, that is, for about 7–10% of all drugs clinically used, although prospective clinical studies are necessary to evaluate the exact benefit of drug selection and dosage.
Journal ArticleDOI
Polymorphism of human cytochrome P450 2D6 and its clinical significance: part II.
TL;DR: There is a considerable variability in the CYP2D6 allele distribution among different ethnic groups, resulting in variable percentages of PMs, IMs, EMs and UMs in a given population and the number of alleles is still growing.
Journal ArticleDOI
Pharmacogenetics of antidepressants and antipsychotics: the contribution of allelic variations to the phenotype of drug response
Julia Kirchheiner,K. Nickchen,Michael Bauer,Ma-Li Wong,Julio Licinio,Ivar Roots,Jürgen Brockmöller +6 more
TL;DR: Combinations of polymorphisms in pharmacokinetic and pharmacodynamic pathways of relevance might contribute to identify genotypes associated with best and worst responders and they may also identify susceptibility to adverse drug reactions.
Journal ArticleDOI
Xenobiotic-metabolizing enzymes involved in activation and detoxification of carcinogenic polycyclic aromatic hydrocarbons
TL;DR: Inter-individual differences exist in levels of expression and catalytic activities of a variety of enzymes that activate and/or detoxify PAHs in various organs of humans and these phenomena are thought to be critical in understanding the basis of individual differences in response toPAHs.
References
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Journal ArticleDOI
Aromatase Cytochrome P450, The Enzyme Responsible for Estrogen Biosynthesis*
Evan R. Simpson,Mala Mahendroo,Gary D. Means,Michael W. Kilgore,Margaret M. Hinshelwood,Sandra E. Graham-Lorence,Bilal Amarneh,Yuji Ito,Carolyn R. Fisher,M. Dodson Michael,Carole R. Mendelson,Serdar E. Bulun +11 more
TL;DR: The biosynthesis of estrogens appears to occur throughout the entire vertebrate phylum including mammals, birds, reptiles, amphibians, teleost and elasmobranch fish, and Agnatha, and in the protochordate Amphioxus.
Journal ArticleDOI
CYTOCHROME P-450 3A4: Regulation and Role in Drug Metabolism
TL;DR: Several issues remain to be resolved regarding the catalytic activity of the P-450 3A4 protein, including rate-limiting steps and the need for cytochrome b5, divalent cations, and acidic phospholipid systems for optimal activity.
Journal ArticleDOI
Role of human cytochrome P-450 IIE1 in the oxidation of many low molecular weight cancer suspects
TL;DR: The results collectively indicate that P-450 IIE1 is a major catalyst of the oxidation of benzene, styrene, CCl4, CHCl3, CH2Cl2, CH3Cl, 1,2-dichloropropane, ethylene dichloride, vinyl chloride, vinyl bromide, acrylonitrile, vinyl carbamate, ethylcarbamate, and trichloroethylene.
Journal ArticleDOI
Human Cytochrome P450 Enzymes: A Status Report Summarizing Their Reactions, Substrates, Inducers, and Inhibitors
TL;DR: A status report summarizing their reactions, substrates, Inducers, and Inhibitors is given in this article, with a focus on human CYtochrome P450 enzymes.
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