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MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition

The Journal of pharmacology and experimental therapeutics, 2015-12, Vol.355 (3), p.397-409

2015

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Bioprinted 3D Primary Human Intestinal Tissues Model Aspects of Native Physiology and ADME/Tox Functions

iScience, 2018-04, Vol.2, p.156-167

2018

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Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

Molecular neurodegeneration, 2017-05, Vol.12 (1), p.39-16, Article 39

2017

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Analysis of tau post-translational modifications in rTg4510 mice, a model of tau pathology

Molecular neurodegeneration, 2015-03, Vol.10 (1), p.14-14, Article 14

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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The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Science translational medicine, 2016-11, Vol.8 (363), p.363ra150

2016

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Accuracy of data buoys for measurement of cyanobacteria, chlorophyll, and turbidity in a large lake (Lake Erie, North America): implications for estimation of cyanobacterial bloom parameters from water quality sonde measurements

Environmental science and pollution research international, 2018-09, Vol.25 (25), p.25175-25189

2018

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Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.2983-2992

2017

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Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors

Bioorganic & medicinal chemistry letters, 2022-01, Vol.56, p.128463-128463, Article 128463

2022

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Chronic Treatment with the γ-Secretase Inhibitor LY-411,575 Inhibits β-Amyloid Peptide Production and Alters Lymphopoiesis and Intestinal Cell Differentiation

The Journal of biological chemistry, 2004-03, Vol.279 (13), p.12876-12882

2004

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Rolapitant (SCH 619734): A potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets

Pharmacology, biochemistry and behavior, 2012-07, Vol.102 (1), p.95-100

2012

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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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Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage

Journal of Alzheimer's disease, 2017-01, Vol.59 (4), p.1393-1413

2017

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Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.8806-8817

2015

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The Environmental Responsibility Framework: A Toolbox for Recognizing and Promoting Ecologically Conscious Research

Earth's future, 2023-04, Vol.11 (4), p.n/a

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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Activation of the NPY Y5 receptor regulates both feeding and energy expenditure

American journal of physiology. Regulatory, integrative and comparative physiology, 1999-11, Vol.277 (5), p.1428-R1434

1999

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Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors

European journal of medicinal chemistry, 2016-11, Vol.124, p.36-48

2016

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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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Identification of Presenilin 1-Selective γ-Secretase Inhibitors with Reconstituted γ-Secretase Complexes

Biochemistry (Easton), 2011-06, Vol.50 (22), p.4973-4980

2011

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Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists

Bioorganic & medicinal chemistry letters, 2015-08, Vol.25 (15), p.2958-2962

2015

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In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

Interdisciplinary perspectives on infectious diseases, 2013, Vol.2013 (2013), p.1-14

2013

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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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MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition

Bioprinted 3D Primary Human Intestinal Tissues Model Aspects of Native Physiology and ADME/Tox Functions

Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

Analysis of tau post-translational modifications in rTg4510 mice, a model of tau pathology

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

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

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

Accuracy of data buoys for measurement of cyanobacteria, chlorophyll, and turbidity in a large lake (Lake Erie, North America): implications for estimation of cyanobacterial bloom parameters from water quality sonde measurements

Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors

Chronic Treatment with the γ-Secretase Inhibitor LY-411,575 Inhibits β-Amyloid Peptide Production and Alters Lymphopoiesis and Intestinal Cell Differentiation

Rolapitant (SCH 619734): A potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets

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

Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage

Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

The Environmental Responsibility Framework: A Toolbox for Recognizing and Promoting Ecologically Conscious Research

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

Activation of the NPY Y5 receptor regulates both feeding and energy expenditure

Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors

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

Cyclic Hydroxyamidines as Amide Isosteres: Discovery of Oxadiazolines and Oxadiazines as Potent and Highly Efficacious γ-Secretase Modulators in Vivo

Identification of Presenilin 1-Selective γ-Secretase Inhibitors with Reconstituted γ-Secretase Complexes

Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists

In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

Discovery of a Tetrahydrobenzisoxazole Series of γ‑Secretase Modulators

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