Studies were conducted to evaluate the potential mechanism-based inactivation of recombinant and human liver microsomal CYP2C8 by clinically used drugs. Several tricyclic antidepres-sants, calcium channel blockers, monoamine oxidase inhibi-tors, and various other known CYP3A4 inhibitors exhibited greater inhibition of CYP2C8 (paclitaxel 6-hydroxylation) fol-lowing preincubation, consistent with mechanism-based inac-tivation. Inactivation of recombinant CYP2C8 by phenelzine, amiodarone, verapamil, nortriptyline, fluoxetine, and isoniazid was of the pseudo-first order type and was characterized by respective inactivation kinetic constants (KI and kinact) of 1.
Identifying selective inhibitors of cytochrome P450 isoforms is a useful tool in defining the role o...
In previous studies, gemfibrozil acyl--glucuronide, but not gem-fibrozil, was found to be a mechanis...
Cytochrome P450 (CYP) constitutes a superfamily of heme- containing enzymes that catalyze the oxidat...
To characterize potential mechanism-based inactivation (MBI) of major human drug-metabolizing cytoch...
The definitive version is available at www.blackwell-synergy.comAIMS: To characterize potential mech...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Several protein kinase inhibitors are known to be mechanism-based inhibitors of cytochrome P450 (CYP...
jpet.aspetjournals.org D ow nloaded from JPET #71803 2 a) Running Title: Mechanism-Based Inactivatio...
Cytochrome P450 (CYP) 3A4 is not only the most abundant isoform in human liver but also metabolizes ...
Cytochrome P450 (CYP) 3A4 is not only the most abundant isoform in human liver but also metabolizes ...
Cytochrome P450 (CYP) 3A4 is not only the most abundant isoform in human liver but also metabolizes ...
The inhibition of human cytochrome P450s (CYPs) is one of the most common mechanisms which can lead ...
Identifying selective inhibitors of cytochrome P450 isoforms is a useful tool in defining the role o...
In previous studies, gemfibrozil acyl--glucuronide, but not gem-fibrozil, was found to be a mechanis...
Cytochrome P450 (CYP) constitutes a superfamily of heme- containing enzymes that catalyze the oxidat...
To characterize potential mechanism-based inactivation (MBI) of major human drug-metabolizing cytoch...
The definitive version is available at www.blackwell-synergy.comAIMS: To characterize potential mech...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Consistent with its highest abundance in humans, cytochrome P450 (CYP) 3A is responsible for the met...
Several protein kinase inhibitors are known to be mechanism-based inhibitors of cytochrome P450 (CYP...
jpet.aspetjournals.org D ow nloaded from JPET #71803 2 a) Running Title: Mechanism-Based Inactivatio...
Cytochrome P450 (CYP) 3A4 is not only the most abundant isoform in human liver but also metabolizes ...
Cytochrome P450 (CYP) 3A4 is not only the most abundant isoform in human liver but also metabolizes ...
Cytochrome P450 (CYP) 3A4 is not only the most abundant isoform in human liver but also metabolizes ...
The inhibition of human cytochrome P450s (CYPs) is one of the most common mechanisms which can lead ...
Identifying selective inhibitors of cytochrome P450 isoforms is a useful tool in defining the role o...
In previous studies, gemfibrozil acyl--glucuronide, but not gem-fibrozil, was found to be a mechanis...
Cytochrome P450 (CYP) constitutes a superfamily of heme- containing enzymes that catalyze the oxidat...