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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation

Nature communications, 2021-02, Vol.12 (1), p.815-11, Article 815

2021

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Tau-tubulin kinase 1 phosphorylates TDP-43 at disease-relevant sites and exacerbates TDP-43 pathology

Neurobiology of disease, 2021-12, Vol.161, p.105548-105548, Article 105548

2021

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Progress toward the development of a viable BACE-1 inhibitor

Drug development research, 2009-03, Vol.70 (2), p.101-110

Stachel, Shawn J.

2009

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Maximizing Diversity from a Kinase Screen: Identification of Novel and Selective pan-Trk Inhibitors for Chronic Pain

Journal of medicinal chemistry, 2014-07, Vol.57 (13), p.5800-5816

2014

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Chondroitin Sulfate Promotes Activation of Cathepsin K

The Journal of biological chemistry, 2014-08, Vol.289 (31), p.21562-21572

2014

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Concise Asymmetric Syntheses of Radicicol and Monocillin I

Journal of the American Chemical Society, 2001-11, Vol.123 (44), p.10903-10908

2001

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Identification, structural, and biophysical characterization of a positive modulator of human Kv3.1 channels

Proceedings of the National Academy of Sciences - PNAS, 2023-10, Vol.120 (42), p.e2220029120-e2220029120

2023

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Lead optimization of cathepsin K inhibitors for the treatment of Osteoarthritis

Bioorganic & medicinal chemistry letters, 2022-10, Vol.74, p.128927-128927, Article 128927

2022

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Total Synthesis as a Resource in the Discovery of Potentially Valuable Antitumor Agents: Cycloproparadicicol

Angewandte Chemie (International ed.), 2003-03, Vol.42 (11), p.1280-1284

2003

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Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors

Bioorganic & medicinal chemistry letters, 2021-07, Vol.44, p.128082, Article 128082

2021

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2‑Aminopyridines as Potent and Selective Nav1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model

ACS medicinal chemistry letters, 2024-06, Vol.15 (6), p.917-923

2024

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Identification and in Vivo Evaluation of Liver X Receptor β‑Selective Agonists for the Potential Treatment of Alzheimer’s Disease

Journal of medicinal chemistry, 2016-04, Vol.59 (7), p.3489-3498

2016

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Biochemical and cell-based assays for characterization of BACE-1 inhibitors

Analytical biochemistry, 2005-07, Vol.342 (1), p.144-151

2005

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Identification of potent inhibitors of the sortilin-progranulin interaction

Bioorganic & medicinal chemistry letters, 2020-09, Vol.30 (17), p.127403-127403, Article 127403

2020

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Structure-Based Design of Potent and Selective Cell-Permeable Inhibitors of Human β-Secretase (BACE-1)

Journal of medicinal chemistry, 2004-12, Vol.47 (26), p.6447-6450

2004

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Development of a pharmacodynamic biomarker to measure target engagement from inhibition of the NGF–TrkA pathway

Journal of neuroscience methods, 2017-04, Vol.282, p.34-42

2017

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The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design

Bioorganic & medicinal chemistry letters, 2017-12, Vol.27 (23), p.5167-5171

2017

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Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species

Bioorganic & medicinal chemistry letters, 2018-04, Vol.28 (6), p.1122-1126

2018

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Preclinical evaluation of [11C]L‐235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone

Journal of labelled compounds & radiopharmaceuticals, 2021-04, Vol.64 (4), p.159-167

2021

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En Route to a Plant Scale Synthesis of the Promising Antitumor Agent 12,13-Desoxyepothilone B

Organic letters, 2000-06, Vol.2 (11), p.1633-1636

2000

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Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor

ACS medicinal chemistry letters, 2018-08, Vol.9 (8), p.815-820

2018

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Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency

Bioorganic & medicinal chemistry letters, 2015-11, Vol.25 (21), p.4812-4819

2015

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Discovery of pyrrolidine-based β-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.240-244

2012

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Identification of a Small Molecule Nonpeptide Active Site β-Secretase Inhibitor That Displays a Nontraditional Binding Mode for Aspartyl Proteases

Journal of medicinal chemistry, 2004-12, Vol.47 (25), p.6117-6119

2004

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Macrocyclic Inhibitors of β-Secretase: Functional Activity in an Animal Model

Journal of medicinal chemistry, 2006-10, Vol.49 (21), p.6147-6150

2006

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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation

Tau-tubulin kinase 1 phosphorylates TDP-43 at disease-relevant sites and exacerbates TDP-43 pathology

Progress toward the development of a viable BACE-1 inhibitor

Maximizing Diversity from a Kinase Screen: Identification of Novel and Selective pan-Trk Inhibitors for Chronic Pain

Chondroitin Sulfate Promotes Activation of Cathepsin K

Concise Asymmetric Syntheses of Radicicol and Monocillin I

Identification, structural, and biophysical characterization of a positive modulator of human Kv3.1 channels

Lead optimization of cathepsin K inhibitors for the treatment of Osteoarthritis

Total Synthesis as a Resource in the Discovery of Potentially Valuable Antitumor Agents: Cycloproparadicicol

Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors

2‑Aminopyridines as Potent and Selective Nav1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model

Identification and in Vivo Evaluation of Liver X Receptor β‑Selective Agonists for the Potential Treatment of Alzheimer’s Disease

Biochemical and cell-based assays for characterization of BACE-1 inhibitors

Identification of potent inhibitors of the sortilin-progranulin interaction

Structure-Based Design of Potent and Selective Cell-Permeable Inhibitors of Human β-Secretase (BACE-1)

Development of a pharmacodynamic biomarker to measure target engagement from inhibition of the NGF–TrkA pathway

The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design

Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species

Preclinical evaluation of [11C]L‐235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone

En Route to a Plant Scale Synthesis of the Promising Antitumor Agent 12,13-Desoxyepothilone B

Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor

Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency

Discovery of pyrrolidine-based β-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency

Identification of a Small Molecule Nonpeptide Active Site β-Secretase Inhibitor That Displays a Nontraditional Binding Mode for Aspartyl Proteases

Macrocyclic Inhibitors of β-Secretase: Functional Activity in an Animal Model

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