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Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators

Bioorganic & medicinal chemistry letters, 2016-11, Vol.26 (21), p.5139-5148

2016

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Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.419-432

2015

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The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: The second clinical candidate having a shorter and favorable human half-life

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7159-7163

2010

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Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators

Biochemical journal, 2016-03, Vol.473 (5), p.581-592

2016

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Crystal structure of human lysosomal acid lipase and its implications in cholesteryl ester storage disease[S]

Journal of lipid research, 2020-08, Vol.61 (8), p.1192-1202

2020

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Structure and Regulation of AMPK

AMP-activated Protein Kinase, 2016, Vol.107, p.3-22

2016

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Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery

Journal of medicinal chemistry, 2019-11, Vol.62 (21), p.9600-9617

2019

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Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging

Angewandte Chemie (International ed.), 2016-08, Vol.55 (33), p.9601-9605

International ed. in English, 2016

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A Novel Mechanism of Cyclooxygenase-2 Inhibition Involving Interactions with Ser-530 and Tyr-385

The Journal of biological chemistry, 2003-11, Vol.278 (46), p.45763-45769

2003

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Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2)

Journal of medicinal chemistry, 2007-05, Vol.50 (11), p.2647-2654

2007

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Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)

Journal of medicinal chemistry, 2018-08, Vol.61 (16), p.7273-7288

2018

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Activation of AMP-Activated Protein Kinase Revealed by Hydrogen/Deuterium Exchange Mass Spectrometry

Structure (London), 2013-11, Vol.21 (11), p.1942-1953

2013

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Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10415-10439

2018

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Discovery of Potent Inhibitors of Soluble Epoxide Hydrolase by Combinatorial Library Design and Structure-Based Virtual Screening

Journal of medicinal chemistry, 2011-03, Vol.54 (5), p.1211-1222

2011

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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.8068-8081

2016

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Molecular Docking and High-Throughput Screening for Novel Inhibitors of Protein Tyrosine Phosphatase-1B

Journal of medicinal chemistry, 2002-05, Vol.45 (11), p.2213-2221

2002

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Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents

Nature (London), 1996-12, Vol.384 (6610), p.644-648

1996

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Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors

Biochemical journal, 2014-06, Vol.460 (2), p.211-222

2014

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Expression and functional characterization of human lysosomal acid lipase gene (LIPA) mutation responsible for cholesteryl ester storage disease (CESD) phenotype

Protein expression and purification, 2015-06, Vol.110, p.22-29

2015

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Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold

Bioorganic & medicinal chemistry letters, 2014-09, Vol.24 (17), p.4132-4140

2014

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Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)

Journal of medicinal chemistry, 2018-03, Vol.61 (6), p.2372-2383

2018

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The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: The first clinical candidate

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7155-7158

2010

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Structural Bioinformatics-Based Prediction of Exceptional Selectivity of p38 MAP Kinase Inhibitor PH-797804

Biochemistry (Easton), 2009-07, Vol.48 (27), p.6402-6411

2009

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Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice

Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators

Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: The second clinical candidate having a shorter and favorable human half-life

Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators

Crystal structure of human lysosomal acid lipase and its implications in cholesteryl ester storage disease[S]

Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms

Structure and Regulation of AMPK

Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery

Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging

A Novel Mechanism of Cyclooxygenase-2 Inhibition Involving Interactions with Ser-530 and Tyr-385

Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2)

Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)

Activation of AMP-Activated Protein Kinase Revealed by Hydrogen/Deuterium Exchange Mass Spectrometry

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist

Discovery of Potent Inhibitors of Soluble Epoxide Hydrolase by Combinatorial Library Design and Structure-Based Virtual Screening

Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy

Molecular Docking and High-Throughput Screening for Novel Inhibitors of Protein Tyrosine Phosphatase-1B

Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents

Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors

Expression and functional characterization of human lysosomal acid lipase gene (LIPA) mutation responsible for cholesteryl ester storage disease (CESD) phenotype

Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)

The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: The first clinical candidate

Structural Bioinformatics-Based Prediction of Exceptional Selectivity of p38 MAP Kinase Inhibitor PH-797804

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