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Human drug metabolising cytochrome P450 enzymes: properties and polymorphisms

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出版社

SPRINGER
DOI: 10.1007/s00210-003-0819-z

关键词

poor metabolizers; adverse drug reactions; genetic polymorphism; haplotypes; cancer drugs; ultrarapid metabolizers

资金

  1. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM060548] Funding Source: NIH RePORTER
  2. NIGMS NIH HHS [1-R01 GM 60548-01A2] Funding Source: Medline

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The cytochrome P450s are responsible for about 75% of phase I dependent drug metabolism and for the metabolism of a huge amount of dietary constituents and endogenous chemicals. The human has 59 active genes, and 6 of those encode important drug metabolising enzymes. About 40% of cytochrome P450 dependent drug metabolism is catalysed by polymorphic enzymes and such drug P450 interactions are frequently seen in adverse drug reaction reports. In this contribution an update of human cytochrome P450 enzymology and pharmacogenetics is given with particular emphasis on CYP1B1, CYP2B6, CYP2E1 and CYP3As.

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