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

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BET Bromodomain Inhibition Releases the Mediator Complex from Select cis -Regulatory Elements

(2016) Anand S. Bhagwat et al.   Cell Reports

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

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

BET bromodomain inhibitors in leukemia

(2015) Faisal Basheer et al.   EXPERIMENTAL HEMATOLOGY

A pooled analysis of overall survival in COMFORT-I and COMFORT-II, 2 randomized phase III trials of ruxolitinib for the treatment of myelofibrosis

(2015) A. M. Vannucchi et al.   HAEMATOLOGICA

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

(2015) S G T Devaraj et al.   LEUKEMIA

BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia

(2015) Jae-Seok Roe et al.   MOLECULAR CELL

NSD3-Short Is an Adaptor Protein that Couples BRD4 to the CHD8 Chromatin Remodeler

(2015) Chen Shen et al.   MOLECULAR CELL

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

(2015) Denes Hnisz et al.   MOLECULAR CELL

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

PIM kinase (and Akt) biology and signaling in tumors

(2015) Noel A. Warfel et al.   PHARMACOLOGY & THERAPEUTICS

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Mass Cytometric Functional Profiling of Acute Myeloid Leukemia Defines Cell-Cycle and Immunophenotypic Properties That Correlate with Known Responses to Therapy

(2015) G. K. Behbehani et al.   Cancer Discovery

A pooled analysis of overall survival in COMFORT-I and COMFORT-II, 2 randomized phase III trials of ruxolitinib for the treatment of myelofibrosis

(2015) A. M. Vannucchi et al.   HAEMATOLOGICA

Integrated genomic analysis illustrates the central role of JAK-STAT pathway activation in myeloproliferative neoplasm pathogenesis

(2014) R. Rampal et al.   BLOOD

MYC through miR-17-92 Suppresses Specific Target Genes to Maintain Survival, Autonomous Proliferation, and a Neoplastic State

(2014) Yulin Li et al.   CANCER CELL

Looping Back to Leap Forward: Transcription Enters a New Era

(2014) Michael Levine et al.   CELL

Molecular Pathways: Molecular Basis for Sensitivity and Resistance to JAK Kinase Inhibitors

(2014) S. C. Meyer et al.   CLINICAL CANCER RESEARCH

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

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 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones

(2014) Tomohiko Kanno et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation

(2014) Friederike Itzen et al.   NUCLEIC ACIDS RESEARCH

Genomic and functional analysis of leukemic transformation of myeloproliferative neoplasms

(2014) Raajit Rampal et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Transcriptional Regulation and Its Misregulation in Disease

(2013) Tong Ihn Lee et al.   CELL

Super-Enhancers in the Control of Cell Identity and Disease

(2013) Denes Hnisz et al.   CELL

Pathogenesis and management of acute myeloid leukemia that has evolved from a myeloproliferative neoplasm

(2013) Raajit Rampal et al.   CURRENT OPINION IN HEMATOLOGY

BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms

(2013) B S Wyspiańska et al.   LEUKEMIA

Dual PI3K/AKT/mTOR Inhibitor BEZ235 Synergistically Enhances the Activity of JAK2 Inhibitor against Cultured and Primary Human Myeloproliferative Neoplasm Cells

(2013) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

The bromodomain protein Brd4 insulates chromatin from DNA damage signalling

(2013) Scott R. Floyd et al.   NATURE

Pim kinases in cancer: Diagnostic, prognostic and treatment opportunities

(2012) Carmen Blanco-Aparicio et al.   BIOCHEMICAL PHARMACOLOGY

Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia

(2012) A. Eghtedar et al.   BLOOD

Genetic analysis of patients with leukemic transformation of myeloproliferative neoplasms shows recurrent SRSF2 mutations that are associated with adverse outcome

(2012) S.-J. Zhang et al.   BLOOD

MYC on the Path to Cancer

(2012) Chi V. Dang   CELL

Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

(2012) Priya Koppikar et al.   NATURE

New mutations and pathogenesis of myeloproliferative neoplasms

(2011) W. Vainchenker et al.   BLOOD

Heat Shock Protein 90 Inhibitor Is Synergistic with JAK2 Inhibitor and Overcomes Resistance to JAK2-TKI in Human Myeloproliferative Neoplasm Cells

(2011) W. Fiskus et al.   CLINICAL CANCER RESEARCH

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Extracting a cellular hierarchy from high-dimensional cytometry data with SPADE

(2011) Peng Qiu et al.   NATURE BIOTECHNOLOGY

Single-Cell Mass Cytometry of Differential Immune and Drug Responses Across a Human Hematopoietic Continuum

(2011) S. C. Bendall et al.   SCIENCE

Transformation of a Chronic Myeloproliferative Neoplasm to Acute Myelogenous Leukemia: Does Anything Work?

(2011) Madappa N. Kundranda et al.   Current Hematologic Malignancy Reports

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

A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations

(2010) Sreenath V. Sharma et al.   CELL

Safety and Efficacy of INCB018424, a JAK1 and JAK2 Inhibitor, in Myelofibrosis

(2010) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

Functional proteomic profiling of AML predicts response and survival

(2008) S. M. Kornblau et al.   BLOOD

Mapping and quantifying mammalian transcriptomes by RNA-Seq

(2008) Ali Mortazavi et al.   NATURE METHODS