Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development

SF Zhou, ZW Zhou, LP Yang… - Current medicinal …, 2009 - ingentaconnect.com
Cytochrome P450 2C9 (CYP2C9) is one of the most abundant CYP enzymes in the human
liver. CYP2C9 metabolizes more than 100 therapeutic drugs, including tolbutamide …

New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I

SL Mo, ZW Zhou, LP Yang, MQ Wei… - Current drug …, 2009 - ingentaconnect.com
CYP2C9 is one of the most abundant CYP enzymes in the human liver (∼ 20% of hepatic
total CYP content). CYP2C9 metabolizes approximately 20% clinical drugs (> 120 drugs) …

Cytochrome P450 2C8: substrates, inhibitors, pharmacogenetics, and clinical relevance

RA Totah, AE Rettie - Clinical Pharmacology & Therapeutics, 2005 - Wiley Online Library
Cytochrome P450 (CYP) 2C9 has been a relatively neglected member of the human CYP2C
family. Over the period from 2000 through 2003, PubMed searches with the key word …

Human CYP2C8: structure, substrate specificity, inhibitor selectivity, inducers and polymorphisms

XS Lai, LP Yang, XT Li, JP Liu, ZW Zhou… - Current drug …, 2009 - ingentaconnect.com
Human CYP2C8 is a key member of the CYP2C family and metabolizes more than 60
clinical drugs. A number of active site residues in CYP2C8 have been identified based on …

Drug metabolism by CYP2C8. 3 is determined by substrate dependent interactions with cytochrome P450 reductase and cytochrome b5

R Kaspera, SB Naraharisetti, EA Evangelista… - Biochemical …, 2011 - Elsevier
Genetic polymorphisms in CYP2C8 can influence the metabolism of important therapeutic
agents and cause interindividual variation in drug response and toxicity. The significance of …

Substrate specificity, inhibitors and regulation of human cytochrome P450 2D6 and implications in drug development

SF Zhou, JP Liu, XS Lai - Current medicinal chemistry, 2009 - ingentaconnect.com
CYP2D6 accounts for only a small percentage of total hepatic CYPs (100) with significant
polymorphisms. A number of drugs acting on the central nervous system and cardiovascular …

CYP2C9 structure− metabolism relationships: substrates, inhibitors, and metabolites

MM Ahlström, M Ridderström… - Journal of medicinal …, 2007 - ACS Publications
The cytochrome P450 (CYP) family is composed of monooxygenases, which mediate the
metabolism of xenobiotics and endogenous compounds. The characterization of the …

Substrate selectivity of human cytochrome P450 2C9: importance of residues 476, 365, and 114 in recognition of diclofenac and sulfaphenazole and in mechanism …

A Melet, N Assrir, P Jean, MP Lopez-Garcia… - Archives of Biochemistry …, 2003 - Elsevier
A series of six site-directed mutants of CYP 2C9 were constructed with the aim to better
define the amino acid residues that play a critical role in substrate selectivity of CYP 2C9 …

PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 8

CL Aquilante, M Niemi, L Gong… - Pharmacogenetics …, 2013 - journals.lww.com
Cytochrome P450, family 2, subfamily C, polypeptide 8 (CYP2C8) is a phase I metabolizing
enzyme that plays an integral role in the biotransformation of structurally diverse xenobiotics …

Clinical and toxicological relevance of CYP2C9: drug-drug interactions and pharmacogenetics

AE Rettie, JP Jones - Annu. Rev. Pharmacol. Toxicol., 2005 - annualreviews.org
▪ Abstract CYP2C9 is a major cytochrome P450 enzyme that is involved in the metabolic
clearance of a wide variety of therapeutic agents, including nonsteroidal antiinflammatories …