Mutate and Conjugate: A Method to Enable Rapid In-Cell Target Validation

Potential applications of clickable probes in EGFR activity visualization and prediction of EGFR-TKI therapy response for NSCLC patients

(2022) Hui Deng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Probability of Success in Drug Development

(2022) Piet H. Graaf   CLINICAL PHARMACOLOGY & THERAPEUTICS

Discovery of Benzo[ d ]imidazole‐6‐sulfonamides as Bromodomain and Extra‐Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain

(2022) Alessandra Cipriano et al.   ChemMedChem

Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432

(2022) Philip G. Humphreys et al.   Journal of Medicinal Chemistry

Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries

(2021) Miljan Kuljanin et al.   NATURE BIOTECHNOLOGY

Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins

(2021) Lee A. Harrison et al.   JOURNAL OF MEDICINAL CHEMISTRY

Substituted 1-methyl-4-phenylpyrrolidin-2-ones – Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors

(2020) J.P. Hilton-Proctor et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

(2020) Omer Gilan et al.   SCIENCE

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

(2020) Robert J. Watson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma

(2020) Renata Rezende Miranda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical epigenetics: the impact of chemical- and chemical biology techniques on bromodomain target validation

(2019) Matthias Schiedel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Trends in clinical success rates and therapeutic focus

(2019) Helen Dowden et al.   NATURE REVIEWS DRUG DISCOVERY

Synthesis and elaboration of N-methylpyrrolidone as an acetamide fragment substitute in bromodomain inhibition

(2019) J.P. Hilton-Proctor et al.   BIOORGANIC & MEDICINAL CHEMISTRY

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability

(2018) Laura E. Jennings et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-based design of targeted covalent inhibitors

(2018) Richard Lonsdale et al.   CHEMICAL SOCIETY REVIEWS

Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition

(2018) A. C. Runcie et al.   Chemical Science

Proteome-wide analysis of cysteine oxidation reveals metabolic sensitivity to redox stress

(2018) Jiska van der Reest et al.   Nature Communications

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

(2018) Matthias Gehringer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3

(2016) Angelina R. Sekirnik née Measures et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions

(2016) Paul A. Jackson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phase II and phase III failures: 2013–2015

(2016) Richard K. Harrison   NATURE REVIEWS DRUG DISCOVERY

The impact of CRISPR–Cas9 on target identification and validation

(2015) Jonathan D. Moore   DRUG DISCOVERY TODAY

Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

(2015) Renato A. Bauer   DRUG DISCOVERY TODAY

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands

(2014) Laura E Jennings et al.   Future Medicinal Chemistry

Clinical development success rates for investigational drugs

(2014) Michael Hay et al.   NATURE BIOTECHNOLOGY

A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

(2014) M. G. J. Baud et al.   SCIENCE

FP tethering: a screening technique to rapidly identify compounds that disrupt protein–protein interactions

(2014) Jean M. Lodge et al.   MedChemComm

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

(2013) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Validating therapeutic targets through human genetics

(2013) Robert M. Plenge et al.   NATURE REVIEWS DRUG DISCOVERY

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

(2012) Panagis Filippakopoulos et al.   CELL

The bromodomain interaction module

(2012) Panagis Filippakopoulos et al.   FEBS LETTERS

Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions

(2012) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

(2011) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides

(2011) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

(2011) Martin Philpott et al.   Molecular BioSystems

Getting pharmaceutical R&D back on target

(2011) Mark E Bunnage   Nature Chemical Biology

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE