Repression of BET activity sensitizes homologous recombination–proficient cancers to PARP inhibition

Rational combination therapy with PARP and MEK inhibitors capitalizes on therapeutic liabilities in RAS mutant cancers

(2017) Chaoyang Sun et al.   Science Translational Medicine

BET Inhibitors Suppress ALDH Activity by Targeting ALDH1A1 Super-Enhancer in Ovarian Cancer

(2016) Yuhki Yokoyama et al.   CANCER RESEARCH

Drug-Driven Synthetic Lethality: Bypassing Tumor Cell Genetics with a Combination of AsiDNA and PARP Inhibitors

(2016) Wael Jdey et al.   CLINICAL CANCER RESEARCH

Replication fork stability confers chemoresistance in BRCA-deficient cells

(2016) Arnab Ray Chaudhuri et al.   NATURE

Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer

(2016) Shaokun Shu et al.   NATURE

Blocking c-Met–mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors

(2016) Yi Du et al.   NATURE MEDICINE

Adaptive Randomization of Veliparib–Carboplatin Treatment in Breast Cancer

(2016) Hope S. Rugo et al.   NEW ENGLAND JOURNAL OF MEDICINE

Laying a trap to kill cancer cells: PARP inhibitors and their mechanisms of action

(2016) Y. Pommier et al.   Science Translational Medicine

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

(2016) A. Stathis et al.   Cancer Discovery

BRD4 Connects Enhancer Remodeling to Senescence Immune Surveillance

(2016) N. Tasdemir et al.   Cancer Discovery

CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer

(2016) Shawn F. Johnson et al.   Cell Reports

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

(2016) Céline Berthon et al.   Lancet Haematology

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

Synthetic Lethality and Cancer Therapy: Lessons Learned from the Development of PARP Inhibitors

(2015) Christopher J. Lord et al.   Annual Review of Medicine

Poly (ADP-Ribose) Polymerase Inhibitors: Recent Advances and Future Development

(2015) Clare L. Scott et al.   JOURNAL OF CLINICAL ONCOLOGY

Olaparib Monotherapy in Patients With Advanced Cancer and a GermlineBRCA1/2Mutation

(2015) Bella Kaufman et al.   JOURNAL OF CLINICAL ONCOLOGY

Chromatin to Clinic: The Molecular Rationale for PARP1 Inhibitor Function

(2015) Felix Y. Feng et al.   MOLECULAR CELL

Homologous-recombination-deficient tumours are dependent on Polθ-mediated repair

(2015) Raphael Ceccaldi et al.   NATURE

Mammalian polymerase θ promotes alternative NHEJ and suppresses recombination

(2015) Pedro A. Mateos-Gomez et al.   NATURE

REV7 counteracts DNA double-strand break resection and affects PARP inhibition

(2015) Guotai Xu et al.   NATURE

Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma

(2015) Pawel K Mazur et al.   NATURE MEDICINE

DNA-Repair Defects and Olaparib in Metastatic Prostate Cancer

(2015) Joaquin Mateo et al.   NEW ENGLAND JOURNAL OF MEDICINE

Homologous Recombination Deficiency: Exploiting the Fundamental Vulnerability of Ovarian Cancer

(2015) P. A. Konstantinopoulos et al.   Cancer Discovery

Histone deacetylase inhibitor treatment induces ‘BRCAness’ and synergistic lethality with PARP inhibitor and cisplatin against human triple negative breast cancer cells

(2015) Kyungsoo Ha et al.   Oncotarget

Combination cediranib and olaparib versus olaparib alone for women with recurrent platinum-sensitive ovarian cancer: a randomised phase 2 study

(2014) Joyce F Liu et al.   LANCET ONCOLOGY

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma

(2014) Maria Giuseppina Baratta et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PARP1-Driven Poly-ADP-Ribosylation Regulates BRCA1 Function in Homologous Recombination-Mediated DNA Repair

(2014) Y. Hu et al.   Cancer Discovery

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

(2013) Bjoern Chapuy et al.   CANCER CELL

Function of BRCA1 in the DNA Damage Response Is Mediated by ADP-Ribosylation

(2013) Mo Li et al.   CANCER CELL

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

The bromodomain protein Brd4 insulates chromatin from DNA damage signalling

(2013) Scott R. Floyd et al.   NATURE

A Genetic Screen Using the PiggyBac Transposon in Haploid Cells Identifies Parp1 as a Mediator of Olaparib Toxicity

(2013) Stephen J. Pettitt et al.   PLoS One

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition

(2013) Alexandre Puissant et al.   Cancer Discovery

Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors

(2012) J. Murai et al.   CANCER RESEARCH

Synthetic lethality of PARP and NAMPT inhibition in triple-negative breast cancer cells

(2012) Ilirjana Bajrami et al.   EMBO Molecular Medicine

Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins

(2012) W. W. Lockwood et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Loss of 53BP1 Causes PARP Inhibitor Resistance in Brca1 -Mutated Mouse Mammary Tumors

(2012) Janneke E. Jaspers et al.   Cancer Discovery

PI3K Inhibition Impairs BRCA1/2 Expression and Sensitizes BRCA-Proficient Triple-Negative Breast Cancer to PARP Inhibition

(2012) Yasir H. Ibrahim et al.   Cancer Discovery

Combining a PI3K Inhibitor with a PARP Inhibitor Provides an Effective Therapy for BRCA1-Related Breast Cancer

(2012) Ashish Juvekar et al.   Cancer Discovery

Dual Roles of PARP-1 Promote Cancer Growth and Progression

(2012) M. J. Schiewer et al.   Cancer Discovery

Mechanistic Rationale for Inhibition of Poly(ADP-Ribose) Polymerase in ETS Gene Fusion-Positive Prostate Cancer

(2011) J. Chad Brenner et al.   CANCER CELL

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

Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibition

(2011) Neil Johnson et al.   NATURE MEDICINE

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Nonhomologous end joining drives poly(ADP-ribose) polymerase (PARP) inhibitor lethality in homologous recombination-deficient cells

(2011) A. G. Patel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

53BP1 Inhibits Homologous Recombination in Brca1-Deficient Cells by Blocking Resection of DNA Breaks

(2010) Samuel F. Bunting et al.   CELL

Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and advanced breast cancer: a proof-of-concept trial

(2010) Andrew Tutt et al.   LANCET

Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and recurrent ovarian cancer: a proof-of-concept trial

(2010) M William Audeh et al.   LANCET

PTEN Deficiency in Endometrioid Endometrial Adenocarcinomas Predicts Sensitivity to PARP Inhibitors

(2010) K. J. Dedes et al.   Science Translational Medicine

Inhibition of Poly(ADP-Ribose) Polymerase in Tumors fromBRCAMutation Carriers

(2009) Peter C. Fong et al.   NEW ENGLAND JOURNAL OF MEDICINE

Secondary mutations as a mechanism of cisplatin resistance in BRCA2-mutated cancers

(2008) Wataru Sakai et al.   NATURE

Resistance to therapy caused by intragenic deletion in BRCA2

(2008) Stacey L. Edwards et al.   NATURE