Inhibiting the DNA damage response as a therapeutic manoeuvre in cancer

Targeting radiation-resistant hypoxic tumour cells through ATR inhibition

(2012) I M Pires et al.   BRITISH JOURNAL OF CANCER

Chemosensitization of Cancer Cells by KU-0060648, a Dual Inhibitor of DNA-PK and PI-3K

(2012) J. M. Munck et al.   MOLECULAR CANCER THERAPEUTICS

Removal of uracil by uracil DNA glycosylase limits pemetrexed cytotoxicity: overriding the limit with methoxyamine to inhibit base excision repair

(2012) A D Bulgar et al.   Cell Death & Disease

Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation

(2012) E Fokas et al.   Cell Death & Disease

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

Identification of Specific Inhibitors of Human RAD51 Recombinase Using High-Throughput Screening

(2011) Fei Huang et al.   ACS Chemical Biology

The role of PARP in DNA repair and its therapeutic exploitation

(2011) M Javle et al.   BRITISH JOURNAL OF CANCER

A phase I study of the safety and tolerability of olaparib (AZD2281, KU0059436) and dacarbazine in patients with advanced solid tumours

(2011) O A Khan et al.   BRITISH JOURNAL OF CANCER

Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines

(2011) A Peasland et al.   BRITISH JOURNAL OF CANCER

Phase I Study of PARP Inhibitor ABT-888 in Combination with Topotecan in Adults with Refractory Solid Tumors and Lymphomas

(2011) S. Kummar et al.   CANCER RESEARCH

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

PTEN Deletion in Prostate Cancer Cells Does Not Associate with Loss of RAD51 Function: Implications for Radiotherapy and Chemotherapy

(2011) M. Fraser et al.   CLINICAL CANCER RESEARCH

Factors determining DNA double-strand break repair pathway choice in G2 phase

(2011) Atsushi Shibata et al.   EMBO JOURNAL

MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation

(2011) Li Wang et al.   INVESTIGATIONAL NEW DRUGS

Safety and tolerability of the poly(ADP-ribose) polymerase (PARP) inhibitor, olaparib (AZD2281) in combination with topotecan for the treatment of patients with advanced solid tumors: a phase I study

(2011) Jens Samol et al.   INVESTIGATIONAL NEW DRUGS

Enhanced Killing of Cancer Cells by Poly(ADP-ribose) Polymerase Inhibitors and Topoisomerase I Inhibitors Reflects Poisoning of Both Enzymes

(2011) Anand G. Patel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Potent and Selective Inhibitors of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Protein Kinase as Potential Anticancer Agents

(2011) Jean-Damien Charrier et al.   JOURNAL OF MEDICINAL CHEMISTRY

Olaparib in patients with recurrent high-grade serous or poorly differentiated ovarian carcinoma or triple-negative breast cancer: a phase 2, multicentre, open-label, non-randomised study

(2011) Karen A Gelmon et al.   LANCET ONCOLOGY

Response of Human Prostate Cancer Cells and Tumors to Combining PARP Inhibition with Ionizing Radiation

(2011) J. C. Barreto-Andrade et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of PARP-1 by Olaparib (AZD2281) Increases the Radiosensitivity of a Lung Tumor Xenograft

(2011) J. M. Senra et al.   MOLECULAR CANCER THERAPEUTICS

The Clinically Active PARP Inhibitor AG014699 Ameliorates Cardiotoxicity but Does Not Enhance the Efficacy of Doxorubicin, despite Improving Tumor Perfusion and Radiation Response in Mice

(2011) M. Ali et al.   MOLECULAR CANCER THERAPEUTICS

Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR

(2011) Philip M Reaper et al.   Nature Chemical Biology

Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibition

(2011) Neil Johnson et al.   NATURE MEDICINE

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations

(2011) Luis I Toledo et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Targeting the DNA Double Strand Break Repair Machinery in Prostate Cancer

(2011) Fadhel S. Shaheen et al.   PLoS One

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

Epigenetic changes of DNA repair genes in cancer

(2011) C. Lahtz et al.   Journal of Molecular Cell Biology

Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699

(2010) R A Daniel et al.   BRITISH JOURNAL OF CANCER

Mitoxantrone in combination with an inhibitor of DNA-dependent protein kinase: a potential therapy for high risk B-cell chronic lymphocytic leukaemia

(2010) Sarah L. Elliott et al.   BRITISH JOURNAL OF HAEMATOLOGY

Contextual Synthetic Lethality of Cancer Cell Kill Based on the Tumor Microenvironment

(2010) N. Chan et al.   CANCER RESEARCH

Human AP endonuclease 1 (APE1): From mechanistic insights to druggable target in cancer

(2010) Rachel Abbotts et al.   CANCER TREATMENT REVIEWS

The role of RPA2 phosphorylation in homologous recombination in response to replication arrest

(2010) Wei Shi et al.   CARCINOGENESIS

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

(2010) Samuel F. Bunting et al.   CELL

Inhibition of ATM kinase activity does not phenocopy ATM protein disruption

(2010) Serah Choi et al.   CELL CYCLE

Small molecule inhibitors of DNA repair nuclease activities of APE1

(2010) David M. Wilson et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Radiation induced DNA DSBs: Contribution from stalled replication forks?

(2010) Jane V. Harper et al.   DNA REPAIR

Multiple roles of ATM in monitoring and maintaining DNA integrity

(2010) Frederick A. Derheimer et al.   FEBS LETTERS

Poly(ADP)-Ribose Polymerase Inhibition: Frequent Durable Responses inBRCACarrier Ovarian Cancer Correlating With Platinum-Free Interval

(2010) Peter C. Fong et al.   JOURNAL OF CLINICAL ONCOLOGY

Evolution of Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors. From Concept to Clinic

(2010) Dana V. Ferraris   JOURNAL OF MEDICINAL CHEMISTRY

Novel Small-Molecule Inhibitor of Apurinic/Apyrimidinic Endonuclease 1 Blocks Proliferation and Reduces Viability of Glioblastoma Cells

(2010) A. Bapat et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Therapeutic Potential of Poly(ADP-ribose) Polymerase Inhibitor AG014699 in Human Cancers With Mutated or Methylated BRCA1 or BRCA2

(2010) Yvette Drew et al.   JNCI-Journal of the National Cancer Institute

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

Purified human BRCA2 stimulates RAD51-mediated recombination

(2010) Ryan B. Jensen et al.   NATURE

Human BRCA2 protein promotes RAD51 filament formation on RPA-covered single-stranded DNA

(2010) Jie Liu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The breast cancer tumor suppressor BRCA2 promotes the specific targeting of RAD51 to single-stranded DNA

(2010) Tina Thorslund et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

53BP1 loss rescues BRCA1 deficiency and is associated with triple-negative and BRCA-mutated breast cancers

(2010) Peter Bouwman et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

ATR: a master conductor of cellular responses to DNA replication stress

(2010) Rachel Litman Flynn et al.   TRENDS IN BIOCHEMICAL SCIENCES

Repair of ionizing radiation-induced DNA double-strand breaks by non-homologous end-joining

(2009) Brandi L. Mahaney et al.   BIOCHEMICAL JOURNAL

A phase I study of extended dosing with lomeguatrib with temozolomide in patients with advanced melanoma

(2009) R F Kefford et al.   BRITISH JOURNAL OF CANCER

A Phase IB Trial of Intravenous INO-1001 Plus Oral Temozolomide in Subjects with Unresectable Stage-III or IV Melanoma

(2009) Agop Y. Bedikian et al.   CANCER INVESTIGATION

Vasoactivity of AG014699, a Clinically Active Small Molecule Inhibitor of Poly(ADP-ribose) Polymerase: a Contributory Factor to Chemopotentiation In vivo?

(2009) M. Ali et al.   CLINICAL CANCER RESEARCH

Inhibition of Poly(ADP-Ribose) Polymerase-1 Enhances Temozolomide and Topotecan Activity against Childhood Neuroblastoma

(2009) R. A. Daniel et al.   CLINICAL CANCER RESEARCH

In vitro and In vivo Radiosensitization of Glioblastoma Cells by the Poly (ADP-Ribose) Polymerase Inhibitor E7016

(2009) A. L. Russo et al.   CLINICAL CANCER RESEARCH

ABT-888 Confers Broad In vivo Activity in Combination with Temozolomide in Diverse Tumors

(2009) J. P. Palma et al.   CLINICAL CANCER RESEARCH

Colorectal cancer in HNPCC: cumulative lifetime incidence, survival and tumour distribution. A report of 121 families with proven mutations

(2009) E Barrow et al.   CLINICAL GENETICS

PALB2 Links BRCA1 and BRCA2 in the DNA-Damage Response

(2009) Feng Zhang et al.   CURRENT BIOLOGY

PIKK-dependent phosphorylation of Mre11 induces MRN complex inactivation by disassembly from chromatin

(2009) Michela Di Virgilio et al.   DNA REPAIR

Synthetic lethal targeting ofPTENmutant cells with PARP inhibitors

(2009) Ana M. Mendes-Pereira et al.   EMBO Molecular Medicine

Gene-body hypermethylation of ATM in peripheral blood DNA of bilateral breast cancer patients

(2009) James M. Flanagan et al.   HUMAN MOLECULAR GENETICS

Poly(ADP-Ribose) Polymerase-1 and DNA-Dependent Protein Kinase Have Equivalent Roles in Double Strand Break Repair Following Ionizing Radiation

(2009) Jody Mitchell et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

Poly(ADP-ribose) polymerase inhibitor ABT-888 potentiates the cytotoxic activity of temozolomide in leukemia cells: influence of mismatch repair status and O6-methylguanine-DNA methyltransferase activity

(2009) T. M. Horton et al.   MOLECULAR CANCER THERAPEUTICS

Targeting homologous recombination using imatinib results in enhanced tumor cell chemosensitivity and radiosensitivity

(2009) A. Choudhury et al.   MOLECULAR CANCER THERAPEUTICS

Effective sensitization of temozolomide by ABT-888 is lost with development of temozolomide resistance in glioblastoma xenograft lines

(2009) M. J. Clarke et al.   MOLECULAR CANCER THERAPEUTICS

Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion

(2009) S. E. Golding et al.   MOLECULAR CANCER THERAPEUTICS

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

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

Inhibition of ATR protein kinase activity by schisandrin B in DNA damage response

(2009) H. Nishida et al.   NUCLEIC ACIDS RESEARCH

Phosphorylation of Exo1 modulates homologous recombination repair of DNA double-strand breaks

(2009) Emma Bolderson et al.   NUCLEIC ACIDS RESEARCH

A phase II trial of lomeguatrib and temozolomide in metastatic colorectal cancer

(2008) O A Khan et al.   BRITISH JOURNAL OF CANCER

Chronic Hypoxia Decreases Synthesis of Homologous Recombination Proteins to Offset Chemoresistance and Radioresistance

(2008) N. Chan et al.   CANCER RESEARCH

Transient Inhibition of ATM Kinase Is Sufficient to Enhance Cellular Sensitivity to Ionizing Radiation

(2008) M. D. Rainey et al.   CANCER RESEARCH

Secondary BRCA1 Mutations in BRCA1-Mutated Ovarian Carcinomas with Platinum Resistance

(2008) E. M. Swisher et al.   CANCER RESEARCH

Phase I Study of the Poly(ADP-Ribose) Polymerase Inhibitor, AG014699, in Combination with Temozolomide in Patients with Advanced Solid Tumors

(2008) R. Plummer et al.   CLINICAL CANCER RESEARCH

DNA-Dependent Protein Kinase Is a Therapeutic Target and an Indicator of Poor Prognosis in B-Cell Chronic Lymphocytic Leukemia

(2008) E. Willmore et al.   CLINICAL CANCER RESEARCH

A high-throughput RNA interference screen for DNA repair determinants of PARP inhibitor sensitivity

(2008) Christopher J. Lord et al.   DNA REPAIR

A synthetic lethal siRNA screen identifying genes mediating sensitivity to a PARP inhibitor

(2008) Nicholas C Turner et al.   EMBO JOURNAL

Replication-Dependent Radiosensitization of Human Glioma Cells by Inhibition of Poly(ADP-Ribose) Polymerase: Mechanisms and Therapeutic Potential

(2008) Fiona A. Dungey et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

RECQ1 Possesses DNA Branch Migration Activity

(2008) Dmitry V. Bugreev et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1

(2008) Keith A. Menear et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the Treatment of Cancer

(2008) Thomas D. Penning et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Fanconi Anemia Protein FANCM Can Promote Branch Migration of Holliday Junctions and Replication Forks

(2008) Kerstin Gari et al.   MOLECULAR CELL

Identification of Holliday junction resolvases from humans and yeast

(2008) Stephen C. Y. Ip et al.   NATURE

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

A forward chemical genetic screen reveals an inhibitor of the Mre11–Rad50–Nbs1 complex

(2008) Aude Dupré et al.   Nature Chemical Biology

ATR: an essential regulator of genome integrity

(2008) Karlene A. Cimprich et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY