Investigational BET bromodomain protein inhibitors in early stage clinical trials for acute myelogenous leukemia (AML)

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

(2017) D T Saenz et al.   LEUKEMIA

Review: AberrantEVI1expression in acute myeloid leukaemia

(2016) Adil A. Hinai et al.   BRITISH JOURNAL OF HAEMATOLOGY

The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression and Induce Anticancer Effects

(2016) J. Shahbazi et al.   CLINICAL CANCER RESEARCH

Wnt signaling as potential therapeutic target in lung cancer

(2016) Jiali Yang et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies

(2016) G. W. Rhyasen et al.   MOLECULAR CANCER THERAPEUTICS

Roche bets on bromodomains

(2016) Eva von Schaper   NATURE BIOTECHNOLOGY

Functional interdependence of BRD4 and DOT1L in MLL leukemia

(2016) Omer Gilan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Functional interdependence of BRD4 and DOT1L in MLL leukemia

(2016) Omer Gilan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

(2016) Céline Berthon et al.   Lancet Haematology

International phase 3 study of azacitidine vs conventional care regimens in older patients with newly diagnosed AML with >30% blasts

(2015) H. Dombret et al.   BLOOD

Epigenetics and approaches to targeted epigenetic therapy in acute myeloid leukemia

(2015) B. J. Wouters et al.   BLOOD

An update of current treatments for adult acute myeloid leukemia

(2015) H. Dombret et al.   BLOOD

Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies

(2015) Elodie Odore et al.   CLINICAL PHARMACOKINETICS

Transcriptional plasticity promotes primary and acquired resistance to BET inhibition

(2015) Philipp Rathert et al.   NATURE

BET inhibitor resistance emerges from leukaemia stem cells

(2015) Chun Yew Fong et al.   NATURE

BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells

(2015) Marie-Magdelaine Coudé et al.   Oncotarget

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

Differentiation therapy for the treatment of t(8;21) acute myeloid leukemia using histone deacetylase inhibitors

(2014) M. Bots et al.   BLOOD

A Single Oncogenic Enhancer Rearrangement Causes Concomitant EVI1 and GATA2 Deregulation in Leukemia

(2014) Stefan Gröschel et al.   CELL

587 Cellular pharmacokinetics and molecular pharmacodynamics studies of the BRD-BET inhibitor OTX015 in sensitive and resistant leukemic cell lines

(2014) E. Odore et al.   EUROPEAN JOURNAL OF CANCER

Epigenetics in the hematologic malignancies

(2014) C. Y. Fong et al.   HAEMATOLOGICA

Chromatin modifiers and the promise of epigenetic therapy in acute leukemia

(2014) S M Greenblatt et al.   LEUKEMIA

Highly Active Combination of BRD4 Antagonist and Histone Deacetylase Inhibitor against Human Acute Myelogenous Leukemia Cells

(2014) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

BET Protein Antagonist JQ1 Is Synergistically Lethal with FLT3 Tyrosine Kinase Inhibitor (TKI) and Overcomes Resistance to FLT3-TKI in AML Cells Expressing FLT-ITD

(2014) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

Targeting bromodomains: epigenetic readers of lysine acetylation

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

Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation

(2014) Friederike Itzen et al.   NUCLEIC ACIDS RESEARCH

Mutations in epigenetic modifiers in the pathogenesis and therapy of acute myeloid leukemia

(2013) O. Abdel-Wahab et al.   BLOOD

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers

(2013) Anouk Emadali et al.   EMBO Molecular Medicine

BET bromodomain inhibitors: a patent review

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

Cancer-associated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition

(2013) C. Chen et al.   GENES & DEVELOPMENT

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

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

Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia

(2013) M A Dawson et al.   LEUKEMIA

Genomic and Epigenomic Landscapes of Adult De Novo Acute Myeloid Leukemia

(2013)   NEW ENGLAND JOURNAL OF MEDICINE

EZH2 Mutations Are Related to Low Blast Percentage in Bone Marrow and -7/del(7q) in De Novo Acute Myeloid Leukemia

(2013) Xiuli Wang et al.   PLoS One

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia

(2012) C. J. Ott et al.   BLOOD

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

Bromodomain-dependent stage-specific male genome programming by Brdt

(2012) Jonathan Gaucher et al.   EMBO JOURNAL

The bromodomain interaction module

(2012) Panagis Filippakopoulos et al.   FEBS LETTERS

Prognostic Relevance of Integrated Genetic Profiling in Acute Myeloid Leukemia

(2012) Jay P. Patel et al.   NEW ENGLAND JOURNAL OF MEDICINE

BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain

(2012) B. N. Devaiah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

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

Pol II waiting in the starting gates: Regulating the transition from transcription initiation into productive elongation

(2010) Sergei Nechaev et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Distinct clinical and biological features of de novo acute myeloid leukemia with additional sex comb-like 1 (ASXL1) mutations

(2010) W.-C. Chou et al.   BLOOD

FLT3 as a therapeutic target in AML: still challenging after all these years

(2010) T. Kindler et al.   BLOOD

The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting α-Ketoglutarate to 2-Hydroxyglutarate

(2010) Patrick S. Ward et al.   CANCER CELL

IDH1 and IDH2 Mutations Are Frequent Genetic Alterations in Acute Myeloid Leukemia and Confer Adverse Prognosis in Cytogenetically Normal Acute Myeloid Leukemia With NPM1 Mutation Without FLT3 Internal Tandem Duplication

(2010) Peter Paschka et al.   JOURNAL OF CLINICAL ONCOLOGY

Histone deacetylase inhibitors for the treatment of myelodysplastic syndrome and acute myeloid leukemia

(2010) A Quintás-Cardama et al.   LEUKEMIA

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

Recurring Mutations Found by Sequencing an Acute Myeloid Leukemia Genome

(2009) Elaine R. Mardis et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Double Bromodomain Proteins Brd2 and Brd3 Couple Histone Acetylation to Transcription

(2008) Gary LeRoy et al.   MOLECULAR CELL

Mutations and Treatment Outcome in Cytogenetically Normal Acute Myeloid Leukemia

(2008) Richard F. Schlenk et al.   NEW ENGLAND JOURNAL OF MEDICINE