Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition

BET bromodomain inhibitors: a patent review

(2013) Jean-Marc Garnier et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Fragment-Based Drug Discovery of 2-Thiazolidinones as Inhibitors of the Histone Reader BRD4 Bromodomain

(2013) Lele Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

(2013) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Phospho Switch Triggers Brd4 Chromatin Binding and Activator Recruitment for Gene-Specific Targeting

(2013) Shwu-Yuan Wu et al.   MOLECULAR CELL

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

(2013) S. Picaud et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of BET bromodomain inhibitors and their role in target validation

(2013) S. Müller et al.   MedChemComm

Small-Molecule Inhibition of BRDT for Male Contraception

(2012) Martin M. Matzuk et al.   CELL

The bromodomain interaction module

(2012) Panagis Filippakopoulos et al.   FEBS LETTERS

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites

(2012) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

(2012) Paul V. Fish et al.   JOURNAL OF MEDICINAL CHEMISTRY

Place your BETs: the therapeutic potential of bromodomains

(2012) R.K. Prinjha et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Bromodomains: Are Readers Right for Epigenetic Therapy?

(2012) Stuart J. Conway   ACS Medicinal Chemistry Letters

Bromodomains as therapeutic targets

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

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery

(2011) Chun-wa Chung 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

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

(2011) Johannes Zuber et al.   NATURE

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy

(2011) Silviya D. Furdas et al.   MedChemComm

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

The pKBHXDatabase: Toward a Better Understanding of Hydrogen-Bond Basicity for Medicinal Chemists

(2009) Christian Laurence et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pd-Catalyzed Aryl Amination Mediated by Well Defined, N-Heterocyclic Carbene (NHC)–Pd Precatalysts, PEPPSI

(2008) Michael G. Organ et al.   CHEMISTRY-A EUROPEAN JOURNAL