The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)

(2015) Harald Herrmann et al.   Oncotarget

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Super-Enhancers in the Control of Cell Identity and Disease

(2013) Denes Hnisz et al.   CELL

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

(2013) Olivier Mirguet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Remodeling of the Enhancer Landscape during Macrophage Activation Is Coupled to Enhancer Transcription

(2013) Minna U. Kaikkonen et al.   MOLECULAR CELL

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

(2013) Anastasia Wyce et al.   PLoS One

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

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

Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)

(2012) Jonathan Seal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Drug response in a genetically engineered mouse model of multiple myeloma is predictive of clinical efficacy

(2012) M. Chesi et al.   BLOOD

Place your BETs: the therapeutic potential of bromodomains

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

Differentiation of NUT Midline Carcinoma by Epigenomic Reprogramming

(2011) B. E. Schwartz et al.   CANCER RESEARCH

Getting physical in drug discovery II: the impact of chromatographic hydrophobicity measurements and aromaticity

(2011) Robert J. Young et al.   DRUG DISCOVERY TODAY

Bromodomains as therapeutic targets

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

HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

(2011) Omar Khan et al.   IMMUNOLOGY AND CELL BIOLOGY

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

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

(2011) Mark A. Dawson et al.   NATURE

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

(2011) Marcus Bantscheff et al.   NATURE BIOTECHNOLOGY

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

Histone deacetylases as regulators of inflammation and immunity

(2011) Melanie R. Shakespear et al.   TRENDS IN IMMUNOLOGY

Getting physical in drug discovery: a contemporary perspective on solubility and hydrophobicity

(2010) Alan P. Hill et al.   DRUG DISCOVERY TODAY

Biological and Biophysical Properties of the Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid Are Affected by the Presence of Short Alkyl Groups on the Phenyl Ring

(2010) Frédérik Oger et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Chemical phylogenetics of histone deacetylases

(2010) James E Bradner et al.   Nature Chemical Biology

Muscarinic antagonist-β-adrenergic agonist dual pharmacology molecules as bronchodilators: a patent review

(2009) Nicholas C Ray et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Proteomics strategy for quantitative protein interaction profiling in cell extracts

(2009) Kirti Sharma et al.   NATURE METHODS

Chemical target and pathway toxicity mechanisms defined in primary human cell systems

(2009) Ellen L. Berg et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS