Open Access Target Validation Is a More Efficient Way to Accelerate Drug Discovery

Preclinical target validation using patient-derived cells

(2015) Aled M. Edwards et al.   NATURE REVIEWS DRUG DISCOVERY

Human UTY(KDM6C) Is a Male-specificNϵ-Methyl Lysyl Demethylase

(2014) Louise J. Walport et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Patent-free pact pushes the boundaries of precompetitive research

(2014) Elie Dolgin   NATURE MEDICINE

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor

(2013) Agustin H. Mohedas et al.   ACS Chemical Biology

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure

(2013) Priti Anand et al.   CELL

BET acetyl-lysine binding proteins control pathological cardiac hypertrophy

(2013) Jessica I. Spiltoir et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

Open source drug discovery – A limited tutorial

(2013) MURRAY N. ROBERTSON et al.   PARASITOLOGY

A New Class of Small Molecule Inhibitor of BMP Signaling

(2013) Caroline E. Sanvitale et al.   PLoS One

Bromodomain Proteins in HIV Infection

(2013) Daniela Boehm et al.   Viruses-Basel

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

(2012) Guillermo Senisterra et al.   BIOCHEMICAL JOURNAL

The bromodomain interaction module

(2012) Panagis Filippakopoulos et al.   FEBS LETTERS

Structure of the Bone Morphogenetic Protein Receptor ALK2 and Implications for Fibrodysplasia Ossificans Progressiva

(2012) Apirat Chaikuad et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

Epigenetic protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

An Allosteric Inhibitor of Protein Arginine Methyltransferase 3

(2012) Alena Siarheyeva et al.   STRUCTURE

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Short Hairpin RNA Screen Reveals Bromodomain Proteins as Novel Targets in Acute Myeloid Leukemia

(2011) Gerd A. Blobel et al.   CANCER CELL

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Bromodomains as therapeutic targets

(2011) Susanne Muller et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Structural and Evolutionary Basis for the Dual Substrate Selectivity of Human KDM4 Histone Demethylase Family

(2011) Lars Hillringhaus et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Too many roads not taken

(2011) Aled M. Edwards et al.   NATURE

Getting pharmaceutical R&D back on target

(2011) Mark E Bunnage   Nature Chemical Biology

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Reader's block

(2010) Sean D. Taverna et al.   NATURE

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Structural Biology of Human H3K9 Methyltransferases

(2010) Hong Wu et al.   PLoS One

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

(2010) Oliver N. F. King et al.   PLoS One

Open access chemical and clinical probes to support drug discovery

(2009) Aled M Edwards et al.   Nature Chemical Biology

Lessons from 60 years of pharmaceutical innovation

(2009) Bernard Munos   NATURE REVIEWS DRUG DISCOVERY

Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases⊥

(2008) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY