Search Results - "Chan, Tom S."
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Meeting the challenge of predicting hepatic clearance of compounds slowly metabolized by cytochrome P450 using a novel hepatocyte model, HepatoPac
Published in Drug metabolism and disposition (01-12-2013)“…Generating accurate in vitro intrinsic clearance data is an important aspect of predicting in vivo human clearance. Primary hepatocytes in suspension are…”
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Upregulation of Krebs cycle and anaerobic glycolysis activity early after onset of liver ischemia
Published in PloS one (14-06-2018)“…The liver is a highly vascularized organ receiving a dual input of oxygenated blood from the hepatic artery and portal vein. The impact of decreased blood flow…”
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Altered CYP2C9 activity following modulation of CYP3A4 levels in human hepatocytes: an example of protein-protein interactions
Published in Drug metabolism and disposition (01-11-2014)“…Cytochrome P450 (P450) protein-protein interactions resulting in modulation of enzyme activities have been well documented using recombinant isoforms. This…”
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A novel system to determine activity of individual uridine 5′-diphospho-glucuronosyltransferase (UGT) isoforms: Recombinant UGT-beads
Published in The Journal of biological chemistry (01-05-2024)“…Previous work demonstrated that human liver microsomes (HLMs) can spontaneously bind to silica-coated magnetizable beads (HLM-beads) and that these HLM-beads…”
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HLM-beads: Rapid Assessment of Nonspecific Binding to Human Liver Microsomes Using Magnetizable Beads
Published in Drug metabolism and disposition (01-12-2021)“…In early drug development, drug-drug interaction risk is routinely assessed using human liver microsomes (HLMs). Nonspecific binding of drugs to HLMs can…”
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Meeting the Challenge of Predicting Hepatic Clearance of Compounds Slowly Metabolized by Cytochrome P450 Using a Novel Hepatocyte Model, HepatoPac
Published in Drug metabolism and disposition (01-01-2019)“…Generating accurate in vitro intrinsic clearance data is an important aspect of predicting in vivo human clearance. Primary hepatocytes in suspension are…”
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Evaluation of Erythromycin as a Tool to Assess CYP3A Contribution of Low Clearance Compounds in a Long-Term Hepatocyte Culture
Published in Drug metabolism and disposition (01-08-2020)Get full text
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Endogenous and endobiotic induced reactive oxygen species formation by isolated hepatocytes
Published in Free radical biology & medicine (2002)“…The rat hepatocyte catalyzed oxidation of 2′,7′-dichlorofluorescin to form the fluorescent 2,7′-dichlorofluorescein was used to measure endogenous and…”
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Human Liver Microsomes Immobilized on Magnetizable Beads: A Novel Approach to Study In Vitro Drug Metabolism
Published in Drug metabolism and disposition (01-08-2020)“…Human liver microsomes (HLM) are a commonly used tool to study drug metabolism in vitro. Typical experiments conducted using suspensions of HLM can be…”
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Bridging in vitro and in vivo metabolism and transport of faldaprevir in human using a novel cocultured human hepatocyte system, HepatoPac
Published in Drug metabolism and disposition (01-03-2014)“…An increased appreciation of the importance of transporter and enzyme interplay in drug clearance and a desire to delineate these mechanisms necessitates the…”
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Characterization of Divergent Metabolic Pathways in Elucidating an Unexpected, Slow-Forming, and Long Half-Life Major Metabolite of Iclepertin
Published in Pharmaceutical research (01-08-2023)“…Purpose After single oral dosing of the glycine reuptake transporter (GlyT1) inhibitor, iclepertin (BI 425809), a single major circulating metabolite, M530a,…”
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The Absolute Bioavailability, Absorption, Distribution, Metabolism, and Excretion of BI 425809 Administered as an Oral Dose or an Oral Dose with an Intravenous Microtracer Dose of [14C]-BI 425809 in Healthy Males
Published in Clinical drug investigation (01-01-2022)“…Background and Objectives BI 425809, a novel glycine transporter-1 inhibitor, may ameliorate cognitive deficits in schizophrenia. The objectives of the studies…”
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Coenzyme Q cytoprotective mechanisms for mitochondrial complex I cytopathies involves NAD(P)H: quinone oxidoreductase 1(NQO1)
Published in Free radical research (01-04-2002)“…The commonest mitochondrial diseases are probably those impairing the function of complex I of the respiratory electron transport chain. Such complex I…”
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Correction to: The Absolute Bioavailability, Absorption, Distribution, Metabolism, and Excretion of BI 425809 Administered as an Oral Dose or an Oral Dose with an Intravenous Microtracer Dose of [14C]‑BI 425809 in Healthy Males
Published in Clinical drug investigation (01-04-2022)Get full text
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Effects of Cytochrome P450 3A4 Induction and Inhibition on the Pharmacokinetics of BI 425809, a Novel Glycine Transporter 1 Inhibitor
Published in European journal of drug metabolism and pharmacokinetics (01-01-2022)“…Background and Objective Increased glycine availability at the synaptic cleft may enhance N -methyl-D-aspartate receptor signalling and provide a promising…”
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The impact of a CYP2C8-CYP3A4 protein–protein interaction on time dependent inhibition of CYP2C8
Published in Drug metabolism and pharmacokinetics (01-01-2018)Get full text
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The biosynthesis of ascorbate protects isolated rat hepatocytes from cumene hydroperoxide-mediated oxidative stress
Published in Free radical biology & medicine (01-04-2005)“…Most animals synthesize ascorbate. It is an essential enzymatic cofactor for the synthesis of a variety of biological molecules and also a powerful…”
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Considerations from an International Regulatory and Pharmaceutical Industry (IQ MPS Affiliate) Workshop on the Standardization of Complex In Vitro Models in Drug Development
Published in Advanced biology (01-08-2024)“…In May 2022, there is an International Regulatory and Pharmaceutical Industry (Innovation and Quality [IQ] Microphysiological Systems [MPS] Affiliate) Workshop…”
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Glycogenolysis is directed towards ascorbate synthesis by glutathione conjugation
Published in Biochemical and biophysical research communications (23-04-2004)“…Using isolated rat hepatocytes we have shown that glutathione (GSH) depletion by glutathione- S-transferase (GST)-catalyzed conjugation with 1-bromoheptane or…”
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Flavonoid B-Ring Chemistry and Antioxidant Activity: Fast Reaction Kinetics
Published in Biochemical and biophysical research communications (20-04-2001)“…Rapid scavenging of the model stable radical cation, ABTS•+, has been applied to screen for the antioxidant activity of flavonoids. The reaction follows two…”
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