Superior efficacy of cotreatment with BET protein inhibitor and BCL2 or MCL1 inhibitor against AML blast progenitor cells

Enhancer dysfunction in leukemia

(2018) Anand S. Bhagwat et al.   BLOOD

The rise of apoptosis: targeting apoptosis in hematologic malignancies

(2018) Rebecca Valentin et al.   BLOOD

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

(2017) Thorsten Braun et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

(2017) Keith F. McDaniel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enhancing venetoclax activity in acute myeloid leukemia by co-targeting MCL1

(2017) T-C Teh et al.   LEUKEMIA

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

(2017) Georg E. Winter et al.   MOLECULAR CELL

From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

(2017) Avi Ashkenazi et al.   NATURE REVIEWS DRUG DISCOVERY

BET Proteins as Targets for Anticancer Treatment

(2017) Anastasios Stathis et al.   Cancer Discovery

Found in Translation: How Preclinical Research Is Guiding the Clinical Development of the BCL2-Selective Inhibitor Venetoclax

(2017) Joel D. Leverson et al.   Cancer Discovery

Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition

(2017) Joyoti Dey et al.   Scientific Reports

BET protein bromodomain inhibitor-based combinations are highly active against post-myeloproliferative neoplasm secondary AML cells

(2016) D T Saenz et al.   LEUKEMIA

BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members

(2016) S. J. Hogg et al.   MOLECULAR CANCER THERAPEUTICS

HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues

(2016) Xiaoyu Lin et al.   MOLECULAR CANCER THERAPEUTICS

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

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

BCL2 Inhibitors as Anticancer Drugs: A Plethora of Misleading BH3 Mimetics

(2016) R. S. Soderquist et al.   MOLECULAR CANCER THERAPEUTICS

Design and characterization of bivalent BET inhibitors

(2016) Minoru Tanaka et al.   Nature Chemical Biology

Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia

(2016) Andrew W. Roberts et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia

(2016) M. Konopleva et al.   Cancer Discovery

Targeting MCL-1/BCL-XL Forestalls the Acquisition of Resistance to ABT-199 in Acute Myeloid Leukemia

(2016) Kevin H. Lin et al.   Scientific Reports

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

(2016) Céline Berthon et al.   Lancet Haematology

HEXIM1 induction is mechanistically involved in mediating anti-AML activity of BET protein bromodomain antagonist

(2015) S G T Devaraj et al.   LEUKEMIA

Convergence of Developmental and Oncogenic Signaling Pathways at Transcriptional Super-Enhancers

(2015) Denes Hnisz et al.   MOLECULAR CELL

Isocitrate dehydrogenase 1 and 2 mutations induce BCL-2 dependence in acute myeloid leukemia

(2015) Steven M Chan et al.   NATURE MEDICINE

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

(2015) J D Leverson et al.   Cell Death & Disease

Loss in MCL-1 function sensitizes non-Hodgkin’s lymphoma cell lines to the BCL-2-selective inhibitor venetoclax (ABT-199)

(2015) D C Phillips et al.   Blood Cancer Journal

Antiapoptotic potency of Bcl-2 proteins primarily relies on their stability, not binding selectivity

(2014) R. W. Rooswinkel et al.   BLOOD

Acquired mutations in BCL2 family proteins conferring resistance to the BH3 mimetic ABT-199 in lymphoma

(2014) V. Fresquet et al.   BLOOD

BCL-2 family proteins as 5-Azacytidine-sensitizing targets and determinants of response in myeloid malignancies

(2014) J M Bogenberger 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

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

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

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

BCL-2 Inhibition Targets Oxidative Phosphorylation and Selectively Eradicates Quiescent Human Leukemia Stem Cells

(2013) Eleni D. Lagadinou et al.   Cell Stem Cell

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

(2013) M A Dawson et al.   LEUKEMIA

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

Selective BCL-2 Inhibition by ABT-199 Causes On-Target Cell Death in Acute Myeloid Leukemia

(2013) R. Pan et al.   Cancer Discovery

Relative Mitochondrial Priming of Myeloblasts and Normal HSCs Determines Chemotherapeutic Success in AML

(2012) Thanh-Trang Vo et al.   CELL

Phase II Study of Single-Agent Navitoclax (ABT-263) and Biomarker Correlates in Patients with Relapsed Small Cell Lung Cancer

(2012) C. M. Rudin et al.   CLINICAL CANCER RESEARCH

Substantial Susceptibility of Chronic Lymphocytic Leukemia to BCL2 Inhibition: Results of a Phase I Study of Navitoclax in Patients With Relapsed or Refractory Disease

(2011) Andrew W. Roberts et al.   JOURNAL OF CLINICAL ONCOLOGY

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

Pretreatment Mitochondrial Priming Correlates with Clinical Response to Cytotoxic Chemotherapy

(2011) T. N. Chonghaile et al.   SCIENCE

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

Deubiquitinase USP9X stabilizes MCL1 and promotes tumour cell survival

(2009) Martin Schwickart et al.   NATURE