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Detecting reactive drug metabolites for reducing the potential for drug toxicity

Expert opinion on drug metabolism & toxicology, 2015, Vol.11 (8), p.1281-1302

Grillo, Mark P

2015

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Large-scale perfused tissues via synthetic 3D soft microfluidics

Nature communications, 2023-01, Vol.14 (1), p.193-193, Article 193

2023

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In vitro and in vivo pharmacokinetic characterization of mavacamten, a first-in-class small molecule allosteric modulator of beta cardiac myosin

Xenobiotica, 2019-06, Vol.49 (6), p.718-733

2019

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Acyl-CoA thioesters as chemically-reactive intermediates of carboxylic acid-containing drugs

Medicinal chemistry research, 2023-09, Vol.32 (9), p.2058-2070

2023

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Drug-S-acyl-glutathione thioesters: synthesis, bioanalytical properties, chemical reactivity, biological formation and degradation

Current drug metabolism, 2011-03, Vol.12 (3), p.229

Grillo, Mark P

2011

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Effect of culture time on the basal expression levels of drug transporters in sandwich-cultured primary rat hepatocytes

Drug metabolism and disposition, 2011-12, Vol.39 (12), p.2387

2011

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Constituents in Kava Extracts Potentially Involved in Hepatotoxicity: A Review

Chemical research in toxicology, 2011-07, Vol.24 (7), p.992-1002

2011

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Preclinical in vitro and in vivo pharmacokinetic properties of danicamtiv, a new targeted myosin activator for the treatment of dilated cardiomyopathy

Xenobiotica, 2021-02, Vol.51 (2), p.222-238

2021

Volltextzugriff (PDF)

Metabolic activation of carboxylic acids

Expert opinion on drug metabolism & toxicology, 2008-04, Vol.4 (4), p.425-438

2008

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Interaction of γ-glutamyltranspeptidase with ibuprofen-S-acyl-glutathione in vitro and in vivo in human

Drug metabolism and disposition, 2013-01, Vol.41 (1), p.111

2013

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Metabolic activation of mefenamic acid leading to mefenamyl-S-acyl-glutathione adduct formation in vitro and in vivo in rat

Drug metabolism and disposition, 2012-08, Vol.40 (8), p.1515

2012

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Enantioselective Formation of Ibuprofen-S-Acyl-Glutathione in Vitro in Incubations of Ibuprofen with Rat Hepatocytes

Chemical research in toxicology, 2008-09, Vol.21 (9), p.1749-1759

2008

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A novel bioactivation pathway for 2-[2-(2,6-dichlorophenyl)aminophenyl]ethanoic acid (diclofenac) initiated by cytochrome P450-mediated oxidative decarboxylation

Drug metabolism and disposition, 2008-09, Vol.36 (9), p.1740

2008

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Covalent binding of phenylacetic acid to protein in incubations with freshly isolated rat hepatocytes

Drug metabolism and disposition, 2009-05, Vol.37 (5), p.1073

2009

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Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists

Bioorganic & medicinal chemistry letters, 2013-06, Vol.23 (12), p.3609-3613

2013

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Structure-assisted discovery of the first non-retinoid ligands for Retinol-Binding Protein 4

Bioorganic & medicinal chemistry letters, 2014-07, Vol.24 (13), p.2885-2891

2014

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Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists

Bioorganic & medicinal chemistry letters, 2014-01, Vol.24 (1), p.156-160

2014

Volltextzugriff (PDF)

Discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel gpr119 agonists

Bioorganic & medicinal chemistry letters, 2014-02, Vol.24 (4), p.1133-1137

2014

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Studies on the chemical reactivity of diclofenac acyl glucuronide with glutathione: identification of diclofenac-S-acyl-glutathione in rat bile

Drug metabolism and disposition, 2003-11, Vol.31 (11), p.1327

2003

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Studies on the Chemical Reactivity of 2-Phenylpropionic Acid 1-O-Acyl Glucuronide and S-Acyl-CoA Thioester Metabolites

Chemical research in toxicology, 2002-10, Vol.15 (10), p.1309-1317

2002

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Stereoselective flunoxaprofen-S-acyl-glutathione thioester formation mediated by acyl-CoA formation in rat hepatocytes

Drug metabolism and disposition, 2010-01, Vol.38 (1), p.133

2010

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Studies on the reactivity of clofibryl-S-acyl-CoA thioester with glutathione in vitro

Drug metabolism and disposition, 2002-01, Vol.30 (1), p.55

2002

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Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism

Bioorganic & medicinal chemistry letters, 2013-12, Vol.23 (24), p.6625-6628

2013

Volltextzugriff (PDF)

Mechanistic Studies on the Bioactivation of Diclofenac: Identification of Diclofenac-S-acyl-glutathione in Vitro in Incubations with Rat and Human Hepatocytes

Chemical research in toxicology, 2003-11, Vol.16 (11), p.1410-1417

2003

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Identification of zomepirac-S-acyl-glutathione in vitro in incubations with rat hepatocytes and in vivo in rat bile

Drug metabolism and disposition, 2003-11, Vol.31 (11), p.1429

2003

Volltextzugriff (PDF)

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Detecting reactive drug metabolites for reducing the potential for drug toxicity

Large-scale perfused tissues via synthetic 3D soft microfluidics

In vitro and in vivo pharmacokinetic characterization of mavacamten, a first-in-class small molecule allosteric modulator of beta cardiac myosin

Acyl-CoA thioesters as chemically-reactive intermediates of carboxylic acid-containing drugs

Drug-S-acyl-glutathione thioesters: synthesis, bioanalytical properties, chemical reactivity, biological formation and degradation

Effect of culture time on the basal expression levels of drug transporters in sandwich-cultured primary rat hepatocytes

Constituents in Kava Extracts Potentially Involved in Hepatotoxicity: A Review

Preclinical in vitro and in vivo pharmacokinetic properties of danicamtiv, a new targeted myosin activator for the treatment of dilated cardiomyopathy

Metabolic activation of carboxylic acids

Interaction of γ-glutamyltranspeptidase with ibuprofen-S-acyl-glutathione in vitro and in vivo in human

Metabolic activation of mefenamic acid leading to mefenamyl-S-acyl-glutathione adduct formation in vitro and in vivo in rat

Enantioselective Formation of Ibuprofen-S-Acyl-Glutathione in Vitro in Incubations of Ibuprofen with Rat Hepatocytes

A novel bioactivation pathway for 2-[2-(2,6-dichlorophenyl)aminophenyl]ethanoic acid (diclofenac) initiated by cytochrome P450-mediated oxidative decarboxylation

Covalent binding of phenylacetic acid to protein in incubations with freshly isolated rat hepatocytes

Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists

Structure-assisted discovery of the first non-retinoid ligands for Retinol-Binding Protein 4

Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists

Discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel gpr119 agonists

Studies on the chemical reactivity of diclofenac acyl glucuronide with glutathione: identification of diclofenac-S-acyl-glutathione in rat bile

Studies on the Chemical Reactivity of 2-Phenylpropionic Acid 1-O-Acyl Glucuronide and S-Acyl-CoA Thioester Metabolites

Stereoselective flunoxaprofen-S-acyl-glutathione thioester formation mediated by acyl-CoA formation in rat hepatocytes

Studies on the reactivity of clofibryl-S-acyl-CoA thioester with glutathione in vitro

Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism

Mechanistic Studies on the Bioactivation of Diclofenac: Identification of Diclofenac-S-acyl-glutathione in Vitro in Incubations with Rat and Human Hepatocytes

Identification of zomepirac-S-acyl-glutathione in vitro in incubations with rat hepatocytes and in vivo in rat bile

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