BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer

Targeting the cancer epigenome: synergistic therapy with bromodomain inhibitors

(2018) Mahalakshmi Ramadoss et al.   DRUG DISCOVERY TODAY

Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study

(2018) Antoine Italiano et al.   LANCET ONCOLOGY

Enhancer of zeste homolog 2 (EZH2) inhibitors

(2018) Nitya Gulati et al.   LEUKEMIA & LYMPHOMA

First-in-human study of ABBV-075 (mivebresib), a pan-inhibitor of bromodomain and extra terminal (BET) proteins, in patients (pts) with relapsed/refractory (RR) acute myeloid leukemia (AML): Preliminary data.

(2018) Gautam Borthakur et al.   JOURNAL OF CLINICAL ONCOLOGY

EZH2 inhibitors: a patent review (2014-2016)

(2017) Giulia Stazi et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

BET Proteins as Targets for Anticancer Treatment

(2017) Anastasios Stathis et al.   Cancer Discovery

Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628

(2016) A. Stathis et al.   Cancer Discovery

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

(2016) Céline Berthon et al.   Lancet Haematology

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

(2015) Marie-Magdelaine Coudé et al.   Oncotarget

Myc Enforces Overexpression of EZH2 in Early Prostatic Neoplasia via Transcriptional and Post-transcriptional Mechanisms

(2015) Cheryl M. Koh et al.   Oncotarget

Panobinostat plus bortezomib and dexamethasone versus placebo plus bortezomib and dexamethasone in patients with relapsed or relapsed and refractory multiple myeloma: a multicentre, randomised, double-blind phase 3 trial

(2014) Jesús F San-Miguel et al.   LANCET ONCOLOGY

EZH2 overexpression in natural killer/T-cell lymphoma confers growth advantage independently of histone methyltransferase activity

(2013) J. Yan et al.   BLOOD

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

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

Genomic Deregulation of the E2F/Rb Pathway Leads to Activation of the Oncogene EZH2 in Small Cell Lung Cancer

(2013) Bradley P. Coe et al.   PLoS One

The Conserved 12-Amino Acid Stretch in the Inter-Bromodomain Region of BET Family Proteins Functions as a Nuclear Localization Signal

(2012) Hidesuke Fukazawa et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

(2012) Michael T. McCabe et al.   NATURE

Genetic inactivation of the polycomb repressive complex 2 in T cell acute lymphoblastic leukemia

(2012) Panagiotis Ntziachristos et al.   NATURE MEDICINE

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

NUT midline carcinoma

(2010) Christopher Alexander French   CANCER GENETICS AND CYTOGENETICS

Multicenter, Phase II Study of Decitabine for the First-Line Treatment of Older Patients With Acute Myeloid Leukemia

(2009) Amanda F. Cashen et al.   JOURNAL OF CLINICAL ONCOLOGY

Regulation of Aurora B Expression by the Bromodomain Protein Brd4

(2009) J. You et al.   MOLECULAR AND CELLULAR BIOLOGY

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

(2008) Gary LeRoy et al.   MOLECULAR CELL