[HTML][HTML] Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation

UM Zanger, M Schwab - Pharmacology & therapeutics, 2013 - Elsevier
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 …

Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction

M Martignoni, GMM Groothuis… - Expert opinion on drug …, 2006 - Taylor & Francis
Animal models are commonly used in the preclinical development of new drugs to predict
the metabolic behaviour of new compounds in humans. It is, however, important to realise …

Polymorphism of human cytochrome P450 enzymes and its clinical impact

SF Zhou, JP Liu, B Chowbay - Drug metabolism reviews, 2009 - Taylor & Francis
Pharmacogenetics is the study of how interindividual variations in the DNA sequence of
specific genes affect drug response. This article highlights current pharmacogenetic …

The cytochrome P450 superfamily: biochemistry, evolution and drug metabolism in humans

PB Danielson - Current drug metabolism, 2002 - ingentaconnect.com
Cytochrome P450s comprise a superfamily of heme-thiolate proteins named for the spectral
absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in …

Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation

UM Zanger, M Turpeinen, K Klein… - Analytical and bioanalytical …, 2008 - Springer
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 …

[HTML][HTML] Pharmacogenetics of cytochrome P450 2B6 (CYP2B6): advances on polymorphisms, mechanisms, and clinical relevance

UM Zanger, K Klein - Frontiers in genetics, 2013 - frontiersin.org
Cytochrome P450 2B6 (CYP2B6) belongs to the minor drug metabolizing P450s in human
liver. Expression is highly variable both between individuals and within individuals, owing to …

Cytochrome P450 pharmacogenetics and cancer

C Rodriguez-Antona, M Ingelman-Sundberg - Oncogene, 2006 - nature.com
The cytochromes P450 (CYPs) are key enzymes in cancer formation and cancer treatment.
They mediate the metabolic activation of numerous precarcinogens and participate in the …

The cytochrome P450 2B6 (CYP2B6) is the main catalyst of efavirenz primary and secondary metabolism: implication for HIV/AIDS therapy and utility of efavirenz as a …

BA Ward, JC Gorski, DR Jones, SD Hall… - … of Pharmacology and …, 2003 - ASPET
We used human liver microsomes (HLMs) and recombinant cytochromes P450 (P450s) to
identify the routes of efavirenz metabolism and the P450s involved. In HLMs, efavirenz …

Sex is a major determinant of CYP3A4 expression in human liver

R Wolbold, K Klein, O Burk, AK Nüssler, P Neuhaus… - Hepatology, 2003 - journals.lww.com
Many drugs that are substrates of CYP3A4, the major human drug–metabolizing cytochrome
P450 (CYP), show higher clearance in women than in men. Although this effect is believed …

Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study

DW Haas, HJ Ribaudo, RB Kim, C Tierney… - Aids, 2004 - journals.lww.com
Objectives: Efavirenz is an effective antiretroviral agent, but central nervous system side
effects occur commonly, and population (racial) differences in pharmacokinetics and …