CYP2C19 inhibition: the impact of substrate probe selection on in vitro inhibition profiles
RS Foti, JL Wahlstrom - Drug metabolism and disposition, 2008 - ASPET
Understanding the potential for cytochrome P450 (P450)-mediated drug-drug interactions is
a critical part of the drug discovery process. Factors such as nonspecific binding, atypical …
a critical part of the drug discovery process. Factors such as nonspecific binding, atypical …
CYP2C9 inhibition: impact of probe selection and pharmacogenetics on in vitro inhibition profiles
Drug-drug interactions may cause serious adverse events in the clinical setting, and the
cytochromes P450 are the enzyme system most often implicated in these interactions …
cytochromes P450 are the enzyme system most often implicated in these interactions …
Enzyme source effects on CYP2C9 kinetics and inhibition
When choosing a recombinant cytochrome P450 (P450) enzyme system for in vitro studies,
it is critical to understand the strengths, limitations, and applicability of the enzyme system to …
it is critical to understand the strengths, limitations, and applicability of the enzyme system to …
[HTML][HTML] CYP3A probes can quantitatively predict the in vivo kinetics of other CYP3A substrates and can accurately assess CYP3A induction and inhibition
ED Kharasch, KE Thummel… - Molecular …, 2005 - triggered.edina.clockss.org
The activity of cytochromes P450 (CYPs) can be a critical determinant of drug clearance,
and interindividual variability in drug disposition and clinical efficacy. Changes in CYP …
and interindividual variability in drug disposition and clinical efficacy. Changes in CYP …
Multiple, ligand-dependent routes from the active site of cytochrome P450 2C9
V Cojocaru, PJ Winn, RC Wade - Current drug metabolism, 2012 - ingentaconnect.com
The active site of liver-specific, drug-metabolizing cytochrome P450 (CYP)
monooxygenases is deeply buried in the protein and is connected to the protein surface …
monooxygenases is deeply buried in the protein and is connected to the protein surface …
Comparison of cytochrome P450 2C subfamily members in terms of drug oxidation rates and substrate inhibition
T Niwa, H Yamazaki - Current Drug Metabolism, 2012 - ingentaconnect.com
This review focuses on identification of important active-site residues of the cytochrome
P450 2C (CYP2C) subfamily in terms of substrate specificity. A meta-analysis was performed …
P450 2C (CYP2C) subfamily in terms of substrate specificity. A meta-analysis was performed …
Substrate-dependent modulation of CYP3A4 catalytic activity: analysis of 27 test compounds with four fluorometric substrates
DM Stresser, AP Blanchard, SD Turner, JCL Erve… - Drug Metabolism and …, 2000 - ASPET
Inhibition of cytochrome P450 catalytic activity is a principal mechanism for pharmacokinetic
drug-drug interactions. Rapid, in vitro testing for cytochrome P450 inhibition potential is part …
drug-drug interactions. Rapid, in vitro testing for cytochrome P450 inhibition potential is part …
CYP2D6-CYP2C9 protein-protein interactions and isoform-selective effects on substrate binding and catalysis
M Subramanian, M Low, CW Locuson… - Drug metabolism and …, 2009 - ASPET
Cytochrome P450 (P450) protein-protein interactions have been observed with various in
vitro systems. It is interesting to note that these interactions seem to be isoform-dependent …
vitro systems. It is interesting to note that these interactions seem to be isoform-dependent …
Evaluation of CYP2C8 inhibition in vitro: utility of montelukast as a selective CYP2C8 probe substrate
BM VandenBrink, RS Foti, DA Rock, LC Wienkers… - Drug metabolism and …, 2011 - ASPET
Understanding the potential for cytochrome P450 (P450)-mediated drug-drug interactions is
a critical step in the drug discovery process. Although in vitro studies with CYP3A4 …
a critical step in the drug discovery process. Although in vitro studies with CYP3A4 …
Clinical and toxicological relevance of CYP2C9: drug-drug interactions and pharmacogenetics
▪ 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 …
clearance of a wide variety of therapeutic agents, including nonsteroidal antiinflammatories …