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Engineered stabilization and structural analysis of the autoinhibited conformation of PDE4

Proceedings of the National Academy of Sciences - PNAS, 2015-03, Vol.112 (12), p.E1414-E1422

2015

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Cyclic Nucleotide Binding GAF Domains from Phosphodiesterases: Structural and Mechanistic Insights

Structure (London), 2009-12, Vol.17 (12), p.1551-1557

2009

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Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase

Journal of medicinal chemistry, 2017-12, Vol.60 (23), p.9860-9873

2017

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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct

Proceedings of the National Academy of Sciences - PNAS, 2009-10, Vol.106 (43), p.18225-18230

2009

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Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

Current topics in medicinal chemistry, 2013-01, Vol.13 (1), p.26-54

2013

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Design of Selective, ATP-Competitive Inhibitors of Akt

Journal of medicinal chemistry, 2010-06, Vol.53 (12), p.4615-4622

2010

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Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors

Journal of medicinal chemistry, 2007-01, Vol.50 (2), p.182-185

2007

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Synthesis and structure based optimization of novel Akt inhibitors

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3359-3363

2008

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A Novel Binding Mode Reveals Two Distinct Classes of NMDA Receptor GluN2B-selective Antagonists

Molecular pharmacology, 2016-05, Vol.89 (5), p.541-551

2016

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Discovery of Cytotoxic Dolastatin 10 Analogues with N‑Terminal Modifications

Journal of medicinal chemistry, 2014-12, Vol.57 (24), p.10527-10543

2014

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Three-dimensional structures of the periplasmic lysine/arginine/ornithine-binding protein with and without a ligand

The Journal of biological chemistry, 1993-05, Vol.268 (15), p.11348-11355

1993

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Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose

Journal of medicinal chemistry, 2020-11, Vol.63 (22), p.13546-13560

2020

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Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia

Journal of medicinal chemistry, 2009-08, Vol.52 (16), p.5188-5196

2009

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Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1

Journal of medicinal chemistry, 2018-05, Vol.61 (10), p.4635-4640

2018

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Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation

Journal of medicinal chemistry, 2018-04, Vol.61 (7), p.3008-3026

2018

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Three-Dimensional Structure of Dimeric Human Recombinant Macrophage Colony-Stimulating Factor

Science (American Association for the Advancement of Science), 1992-11, Vol.258 (5086), p.1358-1362

1992

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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct

Proceedings of the National Academy of Sciences - PNAS, 2015-06, Vol.106 ((43) ; 10, 2009)

2015

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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.1001-1018

2018

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Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK)

Journal of medicinal chemistry, 2017-09, Vol.60 (18), p.7835-7849

2017

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6-Amino-4-(pyrimidin-4-yl)pyridones: Novel glycogen synthase kinase-3β inhibitors

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1429-1433

2011

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Discovery and Optimization of a Novel Spiropyrrolidine Inhibitor of β-Secretase (BACE1) through Fragment-Based Drug Design

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9069-9088

2012

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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor

Journal of medicinal chemistry, 2017-07, Vol.60 (13), p.5673-5698

2017

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Design, Synthesis, and Cytotoxic Evaluation of Novel Tubulysin Analogues as ADC Payloads

ACS medicinal chemistry letters, 2016-11, Vol.7 (11), p.999-1004

2016

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Engineered stabilization and structural analysis of the autoinhibited conformation of PDE4

Cyclic Nucleotide Binding GAF Domains from Phosphodiesterases: Structural and Mechanistic Insights

Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase

Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct

Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

Design of Selective, ATP-Competitive Inhibitors of Akt

Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors

Synthesis and structure based optimization of novel Akt inhibitors

A Novel Binding Mode Reveals Two Distinct Classes of NMDA Receptor GluN2B-selective Antagonists

Discovery of Cytotoxic Dolastatin 10 Analogues with N‑Terminal Modifications

Three-dimensional structures of the periplasmic lysine/arginine/ornithine-binding protein with and without a ligand

Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose

Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia

Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1

Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation

Utilizing Structures of CYP2D6 and BACE1 Complexes To Reduce Risk of Drug–Drug Interactions with a Novel Series of Centrally Efficacious BACE1 Inhibitors

Three-Dimensional Structure of Dimeric Human Recombinant Macrophage Colony-Stimulating Factor

Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate

Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK)

6-Amino-4-(pyrimidin-4-yl)pyridones: Novel glycogen synthase kinase-3β inhibitors

Discovery and Optimization of a Novel Spiropyrrolidine Inhibitor of β-Secretase (BACE1) through Fragment-Based Drug Design

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor

Design, Synthesis, and Cytotoxic Evaluation of Novel Tubulysin Analogues as ADC Payloads

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