A comprehensive review of UDP-glucuronosyltransferase and esterases for drug development
S Oda, T Fukami, T Yokoi, M Nakajima - Drug metabolism and …, 2015 - Elsevier
UDP-glucuronosyltransferase (UGT) and esterases are recognized as the most important
non-P450 enzymes because of their high contribution to drug metabolism. UGTs catalyze …
non-P450 enzymes because of their high contribution to drug metabolism. UGTs catalyze …
The role of drug metabolizing enzymes in clearance
L Di - Expert opinion on drug metabolism & toxicology, 2014 - Taylor & Francis
Introduction: Metabolism is one of the most important clearance pathways representing the
major clearance route of 75% drugs. The four most common drug metabolizing enzymes …
major clearance route of 75% drugs. The four most common drug metabolizing enzymes …
Exploration and application of a liver-on-a-chip device in combination with modelling and simulation for quantitative drug metabolism studies
L Docci, N Milani, T Ramp, AA Romeo, P Godoy… - Lab on a Chip, 2022 - pubs.rsc.org
Microphysiological systems (MPS) are complex and more physiologically realistic cellular in
vitro tools that aim to provide more relevant human in vitro data for quantitative prediction of …
vitro tools that aim to provide more relevant human in vitro data for quantitative prediction of …
The prediction of drug-glucuronidation parameters in humans: UDP-glucuronosyltransferase enzyme-selective substrate and inhibitor probes for reaction phenotyping …
JO Miners, PI Mackenzie, KM Knights - Drug metabolism reviews, 2010 - Taylor & Francis
Major advances in the characterization of uridine diphosphate (UDP)-
glucuronosyltransferase (UGT) enzyme substrate and inhibitor selectivities and the …
glucuronosyltransferase (UGT) enzyme substrate and inhibitor selectivities and the …
In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans
M Obermeier, M Yao, A Khanna, B Koplowitz… - Drug metabolism and …, 2010 - ASPET
(2 S, 3 R, 4 R, 5 S, 6 R)-2-(3-(4-Ethoxybenzyl)-4-chlorophenyl)-6-hydroxymethyl-tetrahydro-
2 H-pyran-3, 4, 5-triol (dapagliflozin; BMS-512148) is a potent sodium-glucose cotransporter …
2 H-pyran-3, 4, 5-triol (dapagliflozin; BMS-512148) is a potent sodium-glucose cotransporter …
Prediction of Human Metabolic Clearance from In Vitro Systems: Retrospective Analysis and Prospective View
D Hallifax, JA Foster, JB Houston - Pharmaceutical research, 2010 - Springer
Purpose To provide a definitive assessment of prediction of in vivo CL int from human liver in
vitro systems for assessment of typical underprediction. Methods A database of published …
vitro systems for assessment of typical underprediction. Methods A database of published …
Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors
RL Walsky, JN Bauman, K Bourcier, G Giddens… - Drug Metabolism and …, 2012 - ASPET
The measurement of the effect of new chemical entities on human UDP-
glucuronosyltransferase (UGT) marker activities using in vitro experimentation represents an …
glucuronosyltransferase (UGT) marker activities using in vitro experimentation represents an …
Mechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug design
L Di, C Keefer, DO Scott, TJ Strelevitz, G Chang… - European journal of …, 2012 - Elsevier
Metabolic stability of drug candidates are often determined in both liver microsome and
hepatocyte assays. Comparison of intrinsic clearance values between the two assays …
hepatocyte assays. Comparison of intrinsic clearance values between the two assays …
N-glucuronidation of drugs and other xenobiotics by human and animal UDP-glucuronosyltransferases
S Kaivosaari, M Finel, M Koskinen - Xenobiotica, 2011 - Taylor & Francis
Metabolic disposition of drugs and other xenobiotics includes glucuronidation reactions that
are catalyzed by the uridine diphosphate glucuronosyltransferases (UGTs). The most …
are catalyzed by the uridine diphosphate glucuronosyltransferases (UGTs). The most …
Reaction phenotyping: advances in the experimental strategies used to characterize the contribution of drug-metabolizing enzymes
MA Zientek, K Youdim - Drug Metabolism and Disposition, 2015 - ASPET
During the process of drug discovery, the pharmaceutical industry is faced with numerous
challenges. One challenge is the successful prediction of the major routes of human …
challenges. One challenge is the successful prediction of the major routes of human …