BET inhibitors in cancer therapeutics: a patent review

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins

(2016) Brigitt Raux et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation

(2016) Xiaoqian Xue et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Bromodomain: A New Target in Emerging Epigenetic Medicine

(2015) Steven G. Smith et al.   ACS Chemical Biology

Abstract 3524: BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models

(2015) Pascale Lejeune et al.   CANCER RESEARCH

Discovery of Chemical Inhibitors of Human Bromodomains

(2015) Guangtao Zhang et al.   CHEMICAL REVIEWS

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

(2015) Matthias G. J. Baud et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors

(2015) Xu Ran et al.   JOURNAL OF MEDICINAL CHEMISTRY

Privileged Diazepine Compounds and Their Emergence as Bromodomain Inhibitors

(2014) Steven G. Smith et al.   CHEMISTRY & BIOLOGY

BET-ting on chromatin-based therapeutics for heart failure

(2014) Saptarsi M. Haldar et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

Targeting bromodomains: epigenetic readers of lysine acetylation

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

BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure

(2013) Priti Anand et al.   CELL

BET bromodomain inhibitors: a patent review

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

BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms

(2013) B S Wyspiańska et al.   LEUKEMIA

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

(2013) Victor S. Gehling et al.   ACS Medicinal Chemistry Letters

Small-Molecule Inhibition of BRDT for Male Contraception

(2012) Martin M. Matzuk et al.   CELL

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

(2012) Panagis Filippakopoulos et al.   CELL

528 The BRD-inhibitor OTX015 Shows Pre-clinical Activity in Diffuse Large B-cell Lymphoma (DLBCL)

(2012) P. Bonetti et al.   EUROPEAN JOURNAL OF CANCER

BET bromodomain inhibition as a novel strategy for reactivation of HIV-1

(2012) Camellia Banerjee et al.   JOURNAL OF LEUKOCYTE BIOLOGY

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

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

Reactivation of Latent HIV-1 by Inhibition of BRD4

(2012) Jian Zhu et al.   Cell Reports

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

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

(2011) Chun-wa Chung 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

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