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The 'rule of three' for fragment-based drug discovery: where are we now?

Nature reviews. Drug discovery, 2013-08, Vol.12 (8), p.644-644

2013

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Towards quantitative and multiplexed in vivo functional cancer genomics

Nature reviews. Genetics, 2018-12, Vol.19 (12), p.741-755

2018

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Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

Molecular cancer therapeutics, 2017-06, Vol.16 (6), p.1010-1020

2017

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The AMBRA1 E3 ligase adaptor regulates the stability of cyclin D

Nature (London), 2021-04, Vol.592 (7856), p.794-798

2021

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Crystallographic screening using ultra-low-molecular-weight ligands to guide drug design

Drug discovery today, 2019-05, Vol.24 (5), p.1081-1086

2019

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Associations between Patient Global Assessment scores and pain, physical function, and fatigue in rheumatoid arthritis: a post hoc analysis of data from phase 3 trials of tofacitinib

Arthritis research & therapy, 2020-10, Vol.22 (1), p.1-243, Article 243

2020

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An Arntl2-Driven Secretome Enables Lung Adenocarcinoma Metastatic Self-Sufficiency

Cancer cell, 2016-05, Vol.29 (5), p.697-710

2016

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Improved protein-ligand docking using GOLD

Proteins, structure, function, and bioinformatics, 2003-09, Vol.52 (4), p.609-623

2003

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Diverse, High-Quality Test Set for the Validation of Protein−Ligand Docking Performance

Journal of medicinal chemistry, 2007-02, Vol.50 (4), p.726-741

2007

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Multiplexed screens identify RAS paralogues HRAS and NRAS as suppressors of KRAS-driven lung cancer growth

Nature cell biology, 2023-01, Vol.25 (1), p.159-169

2023

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A versatile system to record cell-cell interactions

eLife, 2020-10, Vol.9

2020

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LKB1 drives stasis and C/EBP-mediated reprogramming to an alveolar type II fate in lung cancer

Nature communications, 2022-02, Vol.13 (1), p.1090-19, Article 1090

2022

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Comparing protein-ligand docking programs is difficult

Proteins, structure, function, and bioinformatics, 2005-08, Vol.60 (3), p.325-332

2005

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A multiplexed in vivo approach to identify driver genes in small cell lung cancer

Cell reports (Cambridge), 2023-01, Vol.42 (1), p.111990-111990, Article 111990

2023

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Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function

Nature chemical biology, 2012-11, Vol.8 (11), p.920-925

2012

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Opportunity Knocks: Organic Chemistry for Fragment-Based Drug Discovery (FBDD)

Angewandte Chemie International Edition, 2016-01, Vol.55 (2), p.488-492

International ed. in English, 2016

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Apo and Inhibitor Complex Structures of BACE (β-secretase)

Journal of molecular biology, 2004-10, Vol.343 (2), p.407-416

2004

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Protein−Ligand Docking against Non-Native Protein Conformers

Journal of Chemical Information and Modeling, 2008-11, Vol.48 (11), p.2214-2225

2008

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Virtual Screening Using Protein−Ligand Docking: Avoiding Artificial Enrichment

Journal of Chemical Information and Computer Sciences, 2004-05, Vol.44 (3), p.793-806

2004

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The rise of fragment-based drug discovery

Nature chemistry, 2009-06, Vol.1 (3), p.187-192

2009

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Experiences in fragment-based drug discovery

Trends in pharmacological sciences (Regular ed.), 2012-05, Vol.33 (5), p.224-232

2012

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Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors

Journal of medicinal chemistry, 2006-02, Vol.49 (4), p.1346-1355

2006

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Structural biology in fragment-based drug design

Current opinion in structural biology, 2010-08, Vol.20 (4), p.497-507

2010

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A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA

MedChemComm, 2019-09, Vol.1 (9), p.159-1511

2019

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The 'rule of three' for fragment-based drug discovery: where are we now?

Towards quantitative and multiplexed in vivo functional cancer genomics

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

The AMBRA1 E3 ligase adaptor regulates the stability of cyclin D

Crystallographic screening using ultra-low-molecular-weight ligands to guide drug design

Associations between Patient Global Assessment scores and pain, physical function, and fatigue in rheumatoid arthritis: a post hoc analysis of data from phase 3 trials of tofacitinib

An Arntl2-Driven Secretome Enables Lung Adenocarcinoma Metastatic Self-Sufficiency

Improved protein-ligand docking using GOLD

Diverse, High-Quality Test Set for the Validation of Protein−Ligand Docking Performance

Multiplexed screens identify RAS paralogues HRAS and NRAS as suppressors of KRAS-driven lung cancer growth

Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design

A versatile system to record cell-cell interactions

LKB1 drives stasis and C/EBP-mediated reprogramming to an alveolar type II fate in lung cancer

Comparing protein-ligand docking programs is difficult

A multiplexed in vivo approach to identify driver genes in small cell lung cancer

Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function

Opportunity Knocks: Organic Chemistry for Fragment-Based Drug Discovery (FBDD)

Apo and Inhibitor Complex Structures of BACE (β-secretase)

Protein−Ligand Docking against Non-Native Protein Conformers

Virtual Screening Using Protein−Ligand Docking: Avoiding Artificial Enrichment

The rise of fragment-based drug discovery

Experiences in fragment-based drug discovery

Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors

Structural biology in fragment-based drug design

A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA

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