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Metabolic and Pharmaceutical Aspects of Fluorinated Compounds

Journal of medicinal chemistry, 2020-06, Vol.63 (12), p.6315-6386

2020

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Pharmacodynamics‐based approach for efficacious human dose projection of BMS‐986260, a small molecule transforming growth factor beta receptor 1 inhibitor

Biopharmaceutics & drug disposition, 2021-04, Vol.42 (4), p.137-149

2021

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Preclinical Pharmacokinetics and In Vitro Metabolism of Asunaprevir (BMS-650032), a Potent Hepatitis C Virus NS3 Protease Inhibitor

Journal of pharmaceutical sciences, 2015-09, Vol.104 (9), p.2813-2823

2015

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Role of CYP2A5 in the clearance of nicotine and cotinine: insights from studies on a Cyp2a5-null mouse model

The Journal of pharmacology and experimental therapeutics, 2010-02, Vol.332 (2), p.578-587

2010

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Role of Biotransformation Studies in Minimizing Metabolism-Related Liabilities in Drug Discovery

The AAPS journal, 2008-03, Vol.10 (1), p.178-192

2008

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Stephacidin A and B: Two Structurally Novel, Selective Inhibitors of the Testosterone-Dependent Prostate LNCaP Cells

Journal of the American Chemical Society, 2002-12, Vol.124 (49), p.14556-14557

2002

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Recent Natural Products Based Drug Development: A Pharmaceutical Industry Perspective

Journal of natural products (Washington, D.C.), 1998-08, Vol.61 (8), p.1053-1071

Shu, Yue-Zhong

1998

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A novel ring oxidation of 4- or 5-substituted 2H-oxazole to corresponding 2-oxazolone catalyzed by cytosolic aldehyde oxidase

Drug metabolism and disposition, 2012-09, Vol.40 (9), p.1668-1676

2012

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Discovering Drugs through Biological Transformation: Role of Pharmacologically Active Metabolites in Drug Discovery

Journal of medicinal chemistry, 2004-08, Vol.47 (18), p.4339-4351

2004

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Label-Free Bottom-Up Proteomic Workflow for Simultaneously Assessing the Target Specificity of Covalent Drug Candidates and Their Off-Target Reactivity to Selected Proteins

Chemical research in toxicology, 2016-01, Vol.29 (1), p.109-116

2016

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The pneumotoxin 3-methylindole is a substrate and a mechanism-based inactivator of CYP2A13, a human cytochrome P450 enzyme preferentially expressed in the respiratory tract

Drug metabolism and disposition, 2009-10, Vol.37 (10), p.2018-2027

2009

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Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation

Drug metabolism and disposition, 2010-01, Vol.38 (1), p.5-15

2010

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Preclinical metabolism and disposition of an orally bioavailable macrocyclic FXIa inhibitor

Xenobiotica, 2021-08, Vol.51 (8), p.933-948

2021

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High-Resolution Mass Spectrometry-Based Background Subtraction for Identifying Protein Modifications in a Complex Biological System: Detection of Acetaminophen-Bound Microsomal Proteins Including Argininosuccinate Synthetase

Chemical research in toxicology, 2015-04, Vol.28 (4), p.775-781

2015

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Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists – Exploring C6 and C8 SAR using late-stage functionalization

Bioorganic & medicinal chemistry letters, 2020-12, Vol.30 (23), p.127521-127521, Article 127521

2020

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Identification of glutathione conjugates of acetylene-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5

Drug metabolism and disposition, 2015-04, Vol.43 (4), p.578-589

2015

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Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.681-694

2018

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Identification of Human Liver Microsomal Proteins Adducted by a Reactive Metabolite Using Shotgun Proteomics

Chemical research in toxicology, 2014-09, Vol.27 (9), p.1537-1546

2014

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Rosuvastatin Liver Partitioning in Cynomolgus Monkeys: Measurement In Vivo and Prediction Using In Vitro Monkey Hepatocyte Uptake

Drug metabolism and disposition, 2015-11, Vol.43 (11), p.1788-1794

2015

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Bioactivation of cyclopropyl rings by P450: an observation encountered during the optimisation of a series of hepatitis C virus NS5B inhibitors

Xenobiotica, 2018-12, Vol.48 (12), p.1215-1226

2018

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Development, optimization and implementation of a centralized metabolic soft spot assay

Bioanalysis, 2017-04, Vol.9 (7), p.541-552

2017

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Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey

Drug metabolism and disposition, 2008-12, Vol.36 (12), p.2475-2483

2008

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Bioactivation of 2‑(Alkylthio)-1,3,4-Thiadiazoles and 2‑(Alkylthio)-1,3-Benzothiazoles

Chemical research in toxicology, 2012-12, Vol.25 (12), p.2770-2779

2012

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Metabolic and Pharmaceutical Aspects of Fluorinated Compounds

Pharmacodynamics‐based approach for efficacious human dose projection of BMS‐986260, a small molecule transforming growth factor beta receptor 1 inhibitor

Preclinical Pharmacokinetics and In Vitro Metabolism of Asunaprevir (BMS-650032), a Potent Hepatitis C Virus NS3 Protease Inhibitor

Role of CYP2A5 in the clearance of nicotine and cotinine: insights from studies on a Cyp2a5-null mouse model

Role of Biotransformation Studies in Minimizing Metabolism-Related Liabilities in Drug Discovery

Stephacidin A and B: Two Structurally Novel, Selective Inhibitors of the Testosterone-Dependent Prostate LNCaP Cells

Recent Natural Products Based Drug Development: A Pharmaceutical Industry Perspective

A novel ring oxidation of 4- or 5-substituted 2H-oxazole to corresponding 2-oxazolone catalyzed by cytosolic aldehyde oxidase

Discovering Drugs through Biological Transformation: Role of Pharmacologically Active Metabolites in Drug Discovery

A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist

Label-Free Bottom-Up Proteomic Workflow for Simultaneously Assessing the Target Specificity of Covalent Drug Candidates and Their Off-Target Reactivity to Selected Proteins

The pneumotoxin 3-methylindole is a substrate and a mechanism-based inactivator of CYP2A13, a human cytochrome P450 enzyme preferentially expressed in the respiratory tract

Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation

Preclinical metabolism and disposition of an orally bioavailable macrocyclic FXIa inhibitor

High-Resolution Mass Spectrometry-Based Background Subtraction for Identifying Protein Modifications in a Complex Biological System: Detection of Acetaminophen-Bound Microsomal Proteins Including Argininosuccinate Synthetase

Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists – Exploring C6 and C8 SAR using late-stage functionalization

Identification of glutathione conjugates of acetylene-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

Identification of Human Liver Microsomal Proteins Adducted by a Reactive Metabolite Using Shotgun Proteomics

Rosuvastatin Liver Partitioning in Cynomolgus Monkeys: Measurement In Vivo and Prediction Using In Vitro Monkey Hepatocyte Uptake

Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies

Bioactivation of cyclopropyl rings by P450: an observation encountered during the optimisation of a series of hepatitis C virus NS5B inhibitors

Development, optimization and implementation of a centralized metabolic soft spot assay

Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey

Bioactivation of 2‑(Alkylthio)-1,3,4-Thiadiazoles and 2‑(Alkylthio)-1,3-Benzothiazoles

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