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Targeting SARS-CoV‑2 M3CLpro by HCV NS3/4a Inhibitors: In Silico Modeling and In Vitro Screening

Journal of chemical information and modeling, 2021-02, Vol.61 (2), p.1020-1032

2021

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Discovery of Novel Small-Molecule Inhibitors of SARS-CoV‑2 Main Protease as Potential Leads for COVID-19 Treatment

Journal of chemical information and modeling, 2021-09, Vol.61 (9), p.4745-4757

2021

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Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells

Bioorganic & medicinal chemistry letters, 2020-01, Vol.30 (2), p.126806-126806, Article 126806

2020

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Ribosome-Templated Azide–Alkyne Cycloadditions: Synthesis of Potent Macrolide Antibiotics by In Situ Click Chemistry

Journal of the American Chemical Society, 2016-03, Vol.138 (9), p.3136-3144

2016

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Patient-Derived Phenotypic High-Throughput Assay to Identify Small Molecules Restoring Lysosomal Function in Tay–Sachs Disease

SLAS discovery, 2019-03, Vol.24 (3), p.295-303

2019

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Extracellular Acetylated Histone 3.3 Induces Inflammation and Lung Tissue Damage

Biomolecules (Basel, Switzerland), 2023-08, Vol.13 (9), p.1334

2023

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High-Throughput Ca2+ Flux Assay To Monitor Cyclic Nucleotide-Gated Channel Activity and Characterize Achromatopsia Mutant Channel Function

ACS chemical neuroscience, 2019-08, Vol.10 (8), p.3662-3670

2019

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High-Throughput Ca 2+ Flux Assay To Monitor Cyclic Nucleotide-Gated Channel Activity and Characterize Achromatopsia Mutant Channel Function

ACS chemical neuroscience, 2019-08, Vol.10 (8), p.3662-3670

2019

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Discovery of Imidazole-Based Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase

ACS medicinal chemistry letters, 2021-12, Vol.12 (12), p.1962-1967

2021

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LRRTM3 Promotes Processing of Amyloid-Precursor Protein by BACE1 and Is a Positional Candidate Gene for Late-Onset Alzheimer's Disease

Proceedings of the National Academy of Sciences - PNAS, 2006-11, Vol.103 (47), p.17967-17972

2006

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Fragment-Based Discovery of Nonpeptidic BACE-1 Inhibitors Using Tethering

Biochemistry (Easton), 2009-06, Vol.48 (21), p.4488-4496

2009

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Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.4057-4061

2007

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Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1779-1782

2010

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Patient derived phenotypic high throughput assay to discover treatments for Tay-Sachs disease

Molecular genetics and metabolism, 2017-01, Vol.120 (1-2), p.S70-S70

2017

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Development of a High-Throughput Ca2+ Flux Screening Assay to Monitor Cyclic Nucleotide-Gated Channel Activity and Evaluate Achromatopsia Disease Mutant Channel Function

Biophysical journal, 2019-02, Vol.116 (3), p.107-108a

2019

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Design and Synthesis of 2,3,5-Substituted Imidazolidin-4-one Inhibitors of BACE-1

ChemMedChem, 2007-07, Vol.2 (7), p.995-999

2007

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First Optimization of Novel, Potent, Selective PDE11A4 Inhibitors for Age-Related Cognitive Decline

Journal of medicinal chemistry, 2023-11, Vol.66 (21), p.14597-14608

2023

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Electrochemiluminescence assay for basic carboxypeptidases: inhibition of basic carboxypeptidases and activation of thrombin-activatable fibrinolysis inhibitor

Analytical biochemistry, 2003-08, Vol.319 (1), p.159-170

2003

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Optimization of the β-Aminoester class of factor Xa inhibitors. part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity

Bioorganic & medicinal chemistry letters, 2002-06, Vol.12 (12), p.1671-1674

2002

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Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis

European journal of pharmacology, 2000-02, Vol.389 (2), p.201-207

2000

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Optimization of the β-aminoester class of factor Xa inhibitors. Part 1: P4 and side-chain modifications for improved in vitro potency

Bioorganic & medicinal chemistry letters, 2002-06, Vol.12 (12), p.1667-1670

2002

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First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates

The Journal of pharmacology and experimental therapeutics, 2009-01, Vol.328 (1), p.131

2009

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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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Discovery of Oxadiazoyl Tertiary Carbinamine Inhibitors of β-Secretase (BACE-1)

Journal of medicinal chemistry, 2006-12, Vol.49 (25), p.7270-7273

2006

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Targeting SARS-CoV‑2 M3CLpro by HCV NS3/4a Inhibitors: In Silico Modeling and In Vitro Screening

Discovery of Novel Small-Molecule Inhibitors of SARS-CoV‑2 Main Protease as Potential Leads for COVID-19 Treatment

Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells

Ribosome-Templated Azide–Alkyne Cycloadditions: Synthesis of Potent Macrolide Antibiotics by In Situ Click Chemistry

Patient-Derived Phenotypic High-Throughput Assay to Identify Small Molecules Restoring Lysosomal Function in Tay–Sachs Disease

Extracellular Acetylated Histone 3.3 Induces Inflammation and Lung Tissue Damage

High-Throughput Ca2+ Flux Assay To Monitor Cyclic Nucleotide-Gated Channel Activity and Characterize Achromatopsia Mutant Channel Function

High-Throughput Ca 2+ Flux Assay To Monitor Cyclic Nucleotide-Gated Channel Activity and Characterize Achromatopsia Mutant Channel Function

Discovery of Imidazole-Based Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase

LRRTM3 Promotes Processing of Amyloid-Precursor Protein by BACE1 and Is a Positional Candidate Gene for Late-Onset Alzheimer's Disease

Fragment-Based Discovery of Nonpeptidic BACE-1 Inhibitors Using Tethering

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors

Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors

Patient derived phenotypic high throughput assay to discover treatments for Tay-Sachs disease

Development of a High-Throughput Ca2+ Flux Screening Assay to Monitor Cyclic Nucleotide-Gated Channel Activity and Evaluate Achromatopsia Disease Mutant Channel Function

Design and Synthesis of 2,3,5-Substituted Imidazolidin-4-one Inhibitors of BACE-1

First Optimization of Novel, Potent, Selective PDE11A4 Inhibitors for Age-Related Cognitive Decline

Electrochemiluminescence assay for basic carboxypeptidases: inhibition of basic carboxypeptidases and activation of thrombin-activatable fibrinolysis inhibitor

Optimization of the β-Aminoester class of factor Xa inhibitors. part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity

Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis

Optimization of the β-aminoester class of factor Xa inhibitors. Part 1: P4 and side-chain modifications for improved in vitro potency

First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates

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

Discovery of Oxadiazoyl Tertiary Carbinamine Inhibitors of β-Secretase (BACE-1)

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