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Structure-based design of selective, orally available salt-inducible kinase inhibitors that stimulate bone formation in mice

Proceedings of the National Academy of Sciences - PNAS, 2022-12, Vol.119 (50), p.e2214396119

2022

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Aryl Hydrocarbon Receptor Regulates Cell Cycle Progression in Human Breast Cancer Cells via a Functional Interaction with Cyclin-Dependent Kinase 4

Molecular pharmacology, 2010-02, Vol.77 (2), p.195-201

2010

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Identification of a Selective SCoR2 Inhibitor That Protects Against Acute Kidney Injury

Journal of medicinal chemistry, 2023-04, Vol.66 (8), p.5657-5668

2023

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Activation of the Aryl-Hydrocarbon Receptor Inhibits Invasive and Metastatic Features of Human Breast Cancer Cells and Promotes Breast Cancer Cell Differentiation

Molecular endocrinology (Baltimore, Md.), 2010-02, Vol.24 (2), p.359-369

2010

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Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity

Journal of medicinal chemistry, 2008-06, Vol.51 (11), p.3061-3064

2008

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Epigenetics: Novel Therapeutics Targeting Epigenetics

Journal of medicinal chemistry, 2016-02, Vol.59 (4), p.1247-1248

2016

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Arthur A. Patchett Memorial Issue

Journal of medicinal chemistry, 2023-12, Vol.66 (23), p.15565-15566

2023

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Lead Optimization to Advance Protease-Activated Receptor‑1 Antagonists in Early Discovery

Journal of medicinal chemistry, 2022-04, Vol.65 (7), p.5575-5592

2022

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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Bioorganic & medicinal chemistry letters, 2012-04, Vol.22 (7), p.2444-2449

2012

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Discovery of hydroxy pyrimidine Factor IXa inhibitors

Bioorganic & medicinal chemistry letters, 2020-08, Vol.30 (15), p.127279-127279, Article 127279

2020

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Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents

Journal of medicinal chemistry, 2005-09, Vol.48 (19), p.5884-5887

2005

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Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

Bioorganic & medicinal chemistry letters, 2007-03, Vol.17 (5), p.1376-1380

2007

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Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.235-239

2012

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Development of novel cytoprotective small compounds inhibiting mitochondria-dependent cell death

iScience, 2023-10, Vol.26 (10), p.107916-107916, Article 107916

2023

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Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

Journal of medicinal chemistry, 2010-02, Vol.53 (3), p.942-950

2010

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Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes

Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3290-3296

2011

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Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4

Bioorganic & medicinal chemistry letters, 2015-05, Vol.25 (9), p.1836-1841

2015

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Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9331-9345

2012

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Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

ACS medicinal chemistry letters, 2012-11, Vol.3 (11), p.897-902

2012

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Discovery of a Tetrahydrobenzisoxazole Series of γ‑Secretase Modulators

ACS medicinal chemistry letters, 2017-10, Vol.8 (10), p.1002-1006

2017

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Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4

Bioorganic & medicinal chemistry letters, 2015-08, Vol.25 (16), p.3203-3207

2015

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Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound

Bioorganic & medicinal chemistry letters, 2012-02, Vol.22 (3), p.1335-1339

2012

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Tumor-specific expression of cytochrome P450 CYP1B1

Cancer research (Chicago, Ill.), 1997-07, Vol.57 (14), p.3026-3031

1997

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Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (23), p.5836-5841

2016

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Structure-based design of selective, orally available salt-inducible kinase inhibitors that stimulate bone formation in mice

Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

Aryl Hydrocarbon Receptor Regulates Cell Cycle Progression in Human Breast Cancer Cells via a Functional Interaction with Cyclin-Dependent Kinase 4

Identification of a Selective SCoR2 Inhibitor That Protects Against Acute Kidney Injury

Activation of the Aryl-Hydrocarbon Receptor Inhibits Invasive and Metastatic Features of Human Breast Cancer Cells and Promotes Breast Cancer Cell Differentiation

Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity

Epigenetics: Novel Therapeutics Targeting Epigenetics

Arthur A. Patchett Memorial Issue

Lead Optimization to Advance Protease-Activated Receptor‑1 Antagonists in Early Discovery

Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Discovery of hydroxy pyrimidine Factor IXa inhibitors

Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents

Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia

Development of novel cytoprotective small compounds inhibiting mitochondria-dependent cell death

Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes

Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4

Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

Discovery of a Tetrahydrobenzisoxazole Series of γ‑Secretase Modulators

Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4

Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound

Tumor-specific expression of cytochrome P450 CYP1B1

Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

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