The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151

(2012) Olivier Mirguet et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

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 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

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

(2011) Martin Philpott et al.   Molecular BioSystems

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

The development of benzimidazoles as selective rho kinase inhibitors

(2010) E. Hampton Sessions et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Ligand-Free-Palladium-Catalyzed Direct 4-Arylation of Isoxazoles Using Aryl Bromides

(2009) Yacoub Fall et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY