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- Publications
- Influence
Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.
Cytochromes P450 (CYP) are a major source of variability in drug pharmacokinetics and response. Of 57 putatively functional human CYPs only about a dozen enzymes, belonging to the CYP1, 2, and 3… Expand
Cytochrome P450 2D6: overview and update on pharmacology, genetics, biochemistry
- U. Zanger, S. Raimundo, M. Eichelbaum
- Biology, Medicine
- Naunyn-Schmiedeberg's Archives of Pharmacology
- 2003
Of about one dozen human P450 s that catalyze biotransformations of xenobiotics, CYP2D6 is one of the more important ones based on the number of its drug substrates. It shows a very high degree of… Expand
Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver.
The human cytochrome P450, CYP2B6, is involved in the metabolism of several therapeutically important drugs and environmental or abused toxicants. In this study, we present the first systematic… Expand
The genetic determinants of the CYP3A5 polymorphism.
- E. Hustert, M. Haberl, +13 authors L. Wojnowski
- Biology, Medicine
- Pharmacogenetics
- 1 December 2001
CYP3A proteins comprise a significant portion of the hepatic cytochrome P450 (CYP) protein and they metabolize around 50% of drugs currently in use. The dissection of the individual contributions of… Expand
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation
- U. Zanger, M. Turpeinen, K. Klein, M. Schwab
- Medicine, Chemistry
- Analytical and bioanalytical chemistry
- 10 August 2008
We investigated the elimination routes for the 200 drugs that are sold most often by prescription count in the United States. The majority (78%) of the hepatically cleared drugs were found to be… Expand
Identification of the human cytochromes P450 involved in the oxidative metabolism of "Ecstasy"-related designer drugs.
The human cytochrome P450 (CYP) isozymes catalyzing the oxidative metabolism of the widely abused amphetamine derivatives MDMA (N-methyl-3,4-methylenedioxyamphetamine, "Ecstasy"), MDE (N-ethyl-3,… Expand
Molecular mechanisms of genetic polymorphisms of drug metabolism.
One of the major causes of interindividual variation of drug effects is genetic variation of drug metabolism. Genetic polymorphisms of drug-metabolizing enzymes give rise to distinct subgroups in the… Expand
Potent Mechanism-Based Inhibition of Human CYP2B6 by Clopidogrel and Ticlopidine
- T. Richter, T. Mürdter, +5 authors U. Zanger
- Medicine, Chemistry
- Journal of Pharmacology and Experimental…
- 1 January 2004
The thienopyridine derivatives ticlopidine and clopidogrel are inhibitors of ADP-induced platelet aggregation. Pharmacological activity of these prodrugs depends on cytochrome P450 (P450)-dependent… Expand
Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver
- A. Nies, H. Koepsell, +7 authors E. Schaeffeler
- Biology, Medicine
- Hepatology
- 1 October 2009
An important function of hepatocytes is the biotransformation and elimination of various drugs, many of which are organic cations and are taken up by organic cation transporters (OCTs) of the solute… Expand
Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance.
- U. Zanger, K. Klein, T. Saussele, J. Blievernicht, Marco H. Hofmann, M. Schwab
- Biology, Medicine
- Pharmacogenomics
- 18 July 2007
Polymorphisms in drug-metabolizing enzymes and drug transporters contribute to wide and inheritable variability in drug pharmacokinetics, response and toxicity. One of the less well-studied human… Expand