Comparison of Kinetic Parameters for Drug Oxidation Rates and Substrate Inhibition Potential Mediated by Cytochrome P450 3A4 and 3A5

2008 ◽  
Vol 9 (1) ◽  
pp. 20-33 ◽  
Author(s):  
Hiroshi Yamazaki ◽  
Toshiro Niwa ◽  
Norie Murayama ◽  
Chie Emoto
Keyword(s):  
Cytochrome P450 ◽  
Kinetic Parameters ◽  
Substrate Inhibition ◽  
Cytochrome P450 3A4 ◽  
Oxidation Rates ◽  
Drug Oxidation

scholarly journals Chromatographic assays of drug oxidation by human cytochrome P450 3A4

2009 ◽  
Vol 4 (9) ◽  
pp. 1252-1257 ◽  
Author(s):  
Christal D Sohl ◽  
Qian Cheng ◽  
F Peter Guengerich
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 3A4 ◽  
Human Cytochrome ◽  
Drug Oxidation

scholarly journals Constituents of Indonesian Medicinal Plant Averrhoa bilimbi and Their Cytochrome P450 3A4 and 2D6 Inhibitory Activities

2015 ◽  
Vol 10 (1) ◽  
pp. 1934578X1501000
Author(s):  
Lidyawati Auw ◽  
Subehan ◽  
Sukrasno ◽  
Shigetoshi Kadota ◽  
Yasuhiro Tezuka
Keyword(s):  
Cytochrome P450 ◽  
Medicinal Plant ◽  
Kinetic Parameters ◽  
Competitive Inhibitor ◽  
Cytochrome P450 3A4 ◽  
Strong Inhibition ◽  
No Inhibition ◽  
Dependent Inhibition ◽  
Inhibitory Activities ◽  
New Compounds

As constituents of Averrhoa bilimbi leaves we identified three new compounds (1-3) together with 12 known ones (4-15); their inhibitory activities on cytochrome P450 3A4 (CYP3A4) and 2D6 (CYP2D6) were examined. Among the isolated compounds, the mixture of 1 and 2, and compounds 4 and 9 showed strong inhibition on CYP3A4, but mild or no inhibition on CYP2D6. These compounds revealed the characteristics of 1) time- and concentration-dependent inhibition, 2) requirement of NADPH for the inhibition, 3) no protection by nucleophiles, and 4) suppression of the inhibition by competitive inhibitor. Thus, they are suggested to be mechanism-based inactivators of CYP3A4 and CYP2D6. The kinetic parameters for the inactivation (kinact and KI) were 0.19 min–1 and 36.7 μM for the mixture of 1 and 2, 0.126 min–1 and 10.5 μM for 4, and 0.29 min–1 and 23.4 μM for 9.

scholarly journals CO Binding Kinetics of Human Cytochrome P450 3A4

1995 ◽  
Vol 270 (10) ◽  
pp. 5014-5018 ◽  
Author(s):  
Aditya P. Koley ◽  
Jeroen T. M. Buters ◽  
Richard C. Robinson ◽  
Allen Markowitz ◽  
Fred K. Friedman
Keyword(s):  
Cytochrome P450 ◽  
Binding Kinetics ◽  
Cytochrome P450 3A4 ◽  
Human Cytochrome ◽  
Kinetics Of
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