Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2

Double-Expressor Lymphoma Is Associated with Poor Outcomes after Allogeneic Hematopoietic Cell Transplantation

(2018) Ichiro Kawashima et al.   BIOLOGY OF BLOOD AND MARROW TRANSPLANTATION

A concise review of BCL-2 inhibition in acute myeloid leukemia

(2018) Meera Yogarajah et al.   Expert Review of Hematology

Clinical Impact of the Cell-of-Origin Classification and the MYC/BCL2 Dual Expresser Status in Diffuse Large B-Cell Lymphoma Treated Within Prospective Clinical Trials of the German High-Grade Non-Hodgkin's Lymphoma Study Group

(2017) Annette M. Staiger et al.   JOURNAL OF CLINICAL ONCOLOGY

Relapsed or Refractory Double-Expressor and Double-Hit Lymphomas Have Inferior Progression-Free Survival After Autologous Stem-Cell Transplantation

(2017) Alex F. Herrera et al.   JOURNAL OF CLINICAL ONCOLOGY

Combination of Ibrutinib and ABT-199 in Diffuse Large B-Cell Lymphoma and Follicular Lymphoma

(2017) Hsu-Ping Kuo et al.   MOLECULAR CANCER THERAPEUTICS

BRD3/4 inhibition and FLT3-ligand deprivation target pathways that are essential for the survival of human MLL-AF9+ leukemic cells

(2017) Marco Carretta et al.   PLoS One

Transcriptome analysis of dominant-negative Brd4 mutants identifies Brd4-specific target genes of small molecule inhibitor JQ1

(2017) Tim-Michael Decker et al.   Scientific Reports

Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)

(2016) Robert H. Bradbury et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma

(2016) K T Siu et al.   LEUKEMIA

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

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

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

(2016) Sandy Amorim et al.   Lancet Haematology

MicroRNAs as regulators and mediators of c-MYC function

(2015) Rene Jackstadt et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib

(2015) B. Sun et al.   BLOOD

The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs

(2015) M. Boi et al.   CLINICAL CANCER RESEARCH

MYC-mediated Synthetic Lethality for Treatment of Hematological Malignancies

(2015) Xin Li et al.   CURRENT CANCER DRUG TARGETS

ABT-199, a BH3 mimetic that specifically targets Bcl-2, enhances the antitumor activity of chemotherapy, bortezomib and JQ1 in “double hit” lymphoma cells

(2015) Nadine Johnson-Farley et al.   LEUKEMIA & LYMPHOMA

Concurrent inhibition of MYC and BCL2 is a potentially effective treatment strategy for double hit and triple hit B-cell lymphomas

(2015) Munevver Cinar et al.   LEUKEMIA RESEARCH

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

Inhibition of Bromodomain Proteins for the Treatment of Human Diffuse Large B-cell Lymphoma

(2014) S. E. Trabucco et al.   CLINICAL CANCER RESEARCH

MicroRNAs in B-cell lymphomas: how a complex biology gets more complex

(2014) K Musilova 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

MYC/BCL2 protein coexpression contributes to the inferior survival of activated B-cell subtype of diffuse large B-cell lymphoma and demonstrates high-risk gene expression signatures: a report from The International DLBCL Rituximab-CHOP Consortium Program

(2013) S. Hu et al.   BLOOD

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

(2013) A. Chaidos et al.   BLOOD

Discovery and Characterization of Super-Enhancer-Associated Dependencies in Diffuse Large B Cell Lymphoma

(2013) Bjoern Chapuy et al.   CANCER CELL

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development

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

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

(2013) Anastasia Wyce et al.   PLoS One

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition

(2013) Alexandre Puissant et al.   Cancer Discovery

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

(2012) C. J. Ott et al.   BLOOD

BH3 profiling – Measuring integrated function of the mitochondrial apoptotic pathway to predict cell fate decisions

(2012) Victoria Del Gaizo Moore et al.   CANCER LETTERS

Bcl-2 is a better therapeutic target than c-Myc, but attacking both could be a more effective treatment strategy for B-cell lymphoma with concurrent Bcl-2 and c-Myc overexpression

(2011) Nana Sasaki et al.   EXPERIMENTAL HEMATOLOGY

Increased MYC gene copy number correlates with increased mRNA levels in diffuse large B-cell lymphoma

(2010) C. J. Stasik et al.   HAEMATOLOGICA

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

Involvement of BH3-only proteins in hematologic malignancies

(2008) Junya Kuroda et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Gain of chromosome region 18q21 including the MALT1 gene is associated with the activated B-cell-like gene expression subtype and increased BCL2 gene dosage and protein expression in diffuse large B-cell lymphoma

(2008) J. Dierlamm et al.   HAEMATOLOGICA

Pvt1-encoded microRNAs in oncogenesis

(2008) Gabriele B Beck-Engeser et al.   Retrovirology