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Characterization of novel CSF Tau and ptau biomarkers for Alzheimer's disease

PloS one, 2013-10, Vol.8 (10), p.e76523-e76523

2013

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Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer’s Mouse Phenotypes

Cell reports (Cambridge), 2017-07, Vol.20 (1), p.76-88

2017

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Therapeutic Strategies for Alzheimer’s Disease

Molecular neurobiology, 2008-06, Vol.37 (2-3), p.171-186

2008

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Multicenter, Randomized, Double-Blind, Placebo-Controlled, Single-Ascending Dose Study of the Oral γ-Secretase Inhibitor BMS-708163 (Avagacestat): Tolerability Profile, Pharmacokinetic Parameters, and Pharmacodynamic Markers

Clinical therapeutics, 2012-03, Vol.34 (3), p.654-667

2012

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Amelioration of Alpha-1 Antitrypsin Deficiency Diseases with Genome Editing in Transgenic Mice

Human gene therapy, 2018-08, Vol.29 (8), p.861

2018

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Methylation-Sensitive Restriction Enzyme Quantitative Polymerase Chain Reaction Enables Rapid, Accurate, and Precise Detection of Methylation Status of the Regulatory T Cell (Treg)-Specific Demethylation Region in Primary Human Tregs

The Journal of immunology (1950), 2021-01, Vol.206 (2), p.446-451

2021

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Matrix metalloproteinase–activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity

Molecular cancer therapeutics, 2005-05, Vol.4 (5), p.751-760

2005

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Hyperdynamic microtubules, cognitive deficits, and pathology are improved in tau transgenic mice with low doses of the microtubule-stabilizing agent BMS-241027

The Journal of neuroscience, 2012-05, Vol.32 (21), p.7137-7145

2012

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Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain

Journal of medicinal chemistry, 2022-03, Vol.65 (6), p.4534-4564

2022

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Discovery of (S)‑1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein‑2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain

Journal of medicinal chemistry, 2022-03, Vol.65 (6), p.4457-4480

2022

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Response to "Unexpected mutations after CRISPR-Cas9 editing in vivo"

Nature methods, 2018-04, Vol.15 (4), p.236

2018

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Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (22), p.127530, Article 127530

2020

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Recent progress in the medicinal chemistry of gamma-secretase inhibitors

Current topics in medicinal chemistry, 2008, Vol.8 (1), p.17

2008

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Viable mouse gene ablations that robustly alter brain Aβ levels are rare

BMC neuroscience, 2010-11, Vol.11 (1), p.143-143, Article 143

2010

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Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice

The Journal of neuroscience, 2015-04, Vol.35 (17), p.6931-6936

2015

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Identification of Peptide Substrates for Human MMP-11 (Stromelysin-3) Using Phage Display

The Journal of biological chemistry, 2003-07, Vol.278 (30), p.27820-27827

2003

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Discovery of S3-Truncated, C‑6 Heteroaryl Substituted Aminothiazine β‑Site APP Cleaving Enzyme‑1 (BACE1) Inhibitors

Journal of medicinal chemistry, 2016-09, Vol.59 (18), p.8593-8600

2016

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Pharmacodynamics of selective inhibition of γ-secretase by avagacestat

The Journal of pharmacology and experimental therapeutics, 2013-03, Vol.344 (3), p.686

2013

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A Placebo-Controlled, Multiple Ascending Dose Study to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of Avagacestat (BMS-708163) in Healthy Young and Elderly Subjects

Clinical pharmacokinetics, 2012-10, Vol.51 (10), p.681-693

2012

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Association between GTPase activators for Rho and Ras families

Nature (London), 1992-09, Vol.359 (6391), p.153-154

1992

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Tau transgenic mice as models for cerebrospinal fluid tau biomarkers

Journal of Alzheimer's disease, 2011-01, Vol.24 Suppl 2, p.127

2011

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Synergistic inhibition of Aβ production by combinations of γ-secretase modulators

European journal of pharmacology, 2017-10, Vol.812, p.104-112

2017

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Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9208-9223

2012

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Characterization of novel CSF Tau and ptau biomarkers for Alzheimer's disease

Passive immunization with phospho-tau antibodies reduces tau pathology and functional deficits in two distinct mouse tauopathy models

Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer’s Mouse Phenotypes

Therapeutic Strategies for Alzheimer’s Disease

Multicenter, Randomized, Double-Blind, Placebo-Controlled, Single-Ascending Dose Study of the Oral γ-Secretase Inhibitor BMS-708163 (Avagacestat): Tolerability Profile, Pharmacokinetic Parameters, and Pharmacodynamic Markers

Amelioration of Alpha-1 Antitrypsin Deficiency Diseases with Genome Editing in Transgenic Mice

Methylation-Sensitive Restriction Enzyme Quantitative Polymerase Chain Reaction Enables Rapid, Accurate, and Precise Detection of Methylation Status of the Regulatory T Cell (Treg)-Specific Demethylation Region in Primary Human Tregs

Matrix metalloproteinase–activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity

Hyperdynamic microtubules, cognitive deficits, and pathology are improved in tau transgenic mice with low doses of the microtubule-stabilizing agent BMS-241027

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain

Discovery of (S)‑1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein‑2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain

Response to "Unexpected mutations after CRISPR-Cas9 editing in vivo"

Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite

Recent progress in the medicinal chemistry of gamma-secretase inhibitors

Viable mouse gene ablations that robustly alter brain Aβ levels are rare

Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice

Identification of Peptide Substrates for Human MMP-11 (Stromelysin-3) Using Phage Display

Discovery of S3-Truncated, C‑6 Heteroaryl Substituted Aminothiazine β‑Site APP Cleaving Enzyme‑1 (BACE1) Inhibitors

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat

A Placebo-Controlled, Multiple Ascending Dose Study to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of Avagacestat (BMS-708163) in Healthy Young and Elderly Subjects

Association between GTPase activators for Rho and Ras families

Identification and characterization of a MAPT-targeting locked nucleic acid antisense oligonucleotide therapeutic for tauopathies

Tau transgenic mice as models for cerebrospinal fluid tau biomarkers

Synergistic inhibition of Aβ production by combinations of γ-secretase modulators

Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

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