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Article
Novel Multiplexed High Throughput Screening of Selective Inhibitors for Drug-Metabolizing Enzymes Using Human Hepatocytes
Selective chemical inhibitors are critical for reaction phenoty** to identify drug-metabolizing enzymes that are involved in the elimination of drug candidates. Although relatively selective inhibitors are a...
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Article
Characterization of CYP3A5 Selective Inhibitors for Reaction Phenoty** of Drug Candidates
CYP3A is one of the most important classes of enzymes and is involved in the metabolism of over 70% drugs. While several selective CYP3A4 inhibitors have been identified, the search for a selective CYP3A5 inhi...
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Article
The Role of Alcohol Dehydrogenase in Drug Metabolism: Beyond Ethanol Oxidation
Alcohol dehydrogenases (ADHs) are most known for their roles in oxidation and elimination of ethanol. Although less known, ADHs also play a critical role in the metabolism of a number of drugs and metabolites ...
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Protocol
Determination of Fraction Unbound and Unbound Partition Coefficient to Estimate Intracellular Free Drug Concentration
Intracellular free drug concentrations are critical to develop pharmacokinetic and pharmacodynamic relationships, estimate therapeutic indices, and predict drug–drug interaction potentials. Free drug concentra...
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Article
Comparison of Fraction Unbound Between Liver Homogenate and Hepatocytes at 4°C
Fraction unbound (fu) values obtained from liver or hepatocyte homogenate with equilibrium dialysis (fu,homo) or the hepatocyte partition coefficient method at 4°C (fu,c) are both frequently used to estimate unbo...
