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Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Journal of medicinal chemistry, 2012-08, Vol.55 (16), p.7193-7207

2012

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Modulation of Androgen Receptor Activation Function 2 by Testosterone and Dihydrotestosterone

The Journal of biological chemistry, 2007-08, Vol.282 (35), p.25801-25816

2007

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Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance

Molecular cell, 2004-11, Vol.16 (3), p.425-438

2004

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Structural Determinants of Ligand Binding Selectivity between the Peroxisome Proliferator-Activated Receptors

Proceedings of the National Academy of Sciences - PNAS, 2001-11, Vol.98 (24), p.13919-13924

2001

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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists

Journal of medicinal chemistry, 2010-04, Vol.53 (8), p.3412-3416

2010

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Probing the Functional Link between Androgen Receptor Coactivator and Ligand-binding Sites in Prostate Cancer and Androgen Insensitivity

The Journal of biological chemistry, 2006-03, Vol.281 (10), p.6648-6663

2006

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Prevention of Chemotherapy-Induced Alopecia in Rats by CDK Inhibitors

Science (American Association for the Advancement of Science), 2001-01, Vol.291 (5501), p.134-137

2001

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A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors

Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128113-128113, Article 128113

2021

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Structure-Based Design of Potent Retinoid X Receptor α Agonists

Journal of medicinal chemistry, 2004-04, Vol.47 (8), p.2010-2029

2004

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BacMam production and crystal structure of nonglycosylated apo human furin at 1.89 Å resolution

Acta crystallographica. Section F, Structural biology communications, 2019-04, Vol.75 (4), p.239-245

2019

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Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix

Genes & development, 2000-09, Vol.14 (17), p.2229-2241

2000

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Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

Bioorganic & medicinal chemistry letters, 2006-02, Vol.16 (4), p.978-983

2006

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Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis

Journal of medicinal chemistry, 2001-12, Vol.44 (25), p.4339-4358

2001

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Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators

Bioorganic & medicinal chemistry letters, 2010-02, Vol.20 (4), p.1399-1404

2010

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Structure of Rev-erbalpha bound to N-CoR reveals a unique mechanism of nuclear receptor-co-repressor interaction

Nature structural & molecular biology, 2010-07, Vol.17 (7), p.808

2010

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Solution Structure of the Human pp60c-src SH2 Domain Complexed with a Phosphorylated Tyrosine Pentapeptide

Biochemistry (Easton), 1995-02, Vol.34 (7), p.2107-2121

1995

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Catalytic Activity of the SH2 Domain of Human pp60c-src; Evidence from NMR, Mass Spectrometry, Site-Directed Mutagenesis and Kinetic Studies for an Inherent Phosphatase Activity

Biochemistry (Easton), 1995-11, Vol.34 (46), p.15351-15358

1995

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The formation of a covalent complex between a dipeptide ligand and the src SH2 domain

Bioorganic & medicinal chemistry letters, 1998-05, Vol.8 (10), p.1189-1194

1998

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NMR methods for determining the structures of enzyme/inhibitor complexes as an aid in drug design

Biochemical pharmacology, 1990-07, Vol.40 (1), p.161-167

1990

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Heteronuclear three-dimensional NMR spectroscopy applied to CMP-KDO synthetase (27.5 kD)

Biochemical and biophysical research communications, 1989-03, Vol.159 (2), p.842-847

1989

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Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Modulation of Androgen Receptor Activation Function 2 by Testosterone and Dihydrotestosterone

Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance

Structural Determinants of Ligand Binding Selectivity between the Peroxisome Proliferator-Activated Receptors

Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists

Probing the Functional Link between Androgen Receptor Coactivator and Ligand-binding Sites in Prostate Cancer and Androgen Insensitivity

Prevention of Chemotherapy-Induced Alopecia in Rats by CDK Inhibitors

A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors

Structure-Based Design of Potent Retinoid X Receptor α Agonists

BacMam production and crystal structure of nonglycosylated apo human furin at 1.89 Å resolution

Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix

Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis

Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators

Structure of Rev-erbalpha bound to N-CoR reveals a unique mechanism of nuclear receptor-co-repressor interaction

Solution Structure of the Human pp60c-src SH2 Domain Complexed with a Phosphorylated Tyrosine Pentapeptide

Catalytic Activity of the SH2 Domain of Human pp60c-src; Evidence from NMR, Mass Spectrometry, Site-Directed Mutagenesis and Kinetic Studies for an Inherent Phosphatase Activity

The formation of a covalent complex between a dipeptide ligand and the src SH2 domain

NMR methods for determining the structures of enzyme/inhibitor complexes as an aid in drug design

Heteronuclear three-dimensional NMR spectroscopy applied to CMP-KDO synthetase (27.5 kD)

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