Selective PARP1 Inhibitors, PARP1-based Dual-Target Inhibitors, PROTAC PARP1 Degraders, and Prodrugs of PARP1 Inhibitors for Cancer Therapy

Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer

(2022) Shi-Hui Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and Activity of Novel Oxadiazole Based Compounds That Target Poly(ADP-ribose) Polymerase

(2022) Divakar Vishwanath et al.   MOLECULES

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Dual targeting, a new strategy for novel PARP inhibitor discovery

(2022) Lina Wei et al.   Drug Discoveries and Therapeutics

A synergistic interaction between HDAC‐ and PARP inhibitors in childhood tumors with chromothripsis

(2022) Umar Khalid et al.   INTERNATIONAL JOURNAL OF CANCER

PARP inhibition impedes the maturation of nascent DNA strands during DNA replication

(2022) Alina Vaitsiankova et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Cell cycle checkpoints and beyond: Exploiting the ATR/CHK1/WEE1 pathway for the treatment of PARP inhibitor–resistant cancer

(2022) Nitasha Gupta et al.   PHARMACOLOGICAL RESEARCH

STING agonism reprograms tumor-associated macrophages and overcomes resistance to PARP inhibition in BRCA1-deficient models of breast cancer

(2022) Qiwei Wang et al.   Nature Communications

XPO1 inhibition synergizes with PARP1 inhibition in small cell lung cancer by targeting nuclear transport of FOXO3a

(2021) Jingya Wang et al.   CANCER LETTERS

Identification of PARP-7 substrates reveals a role for MARylation in microtubule control in ovarian cancer cells

(2021) Lavanya H Palavalli Parsons et al.   eLife

Alterations of DNA damage response pathway: Biomarker and therapeutic strategy for cancer immunotherapy

(2021) Minlin Jiang et al.   Acta Pharmaceutica Sinica B

Discovery of Novel and Potent PARP/PI3K Dual Inhibitors for the Treatment of Cancer

(2021) Zhengyang Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Contributions of human ACE2 and TMPRSS2 in determining host–pathogen interaction of COVID-19

(2021) SABYASACHI SENAPATI et al.   JOURNAL OF GENETICS

An Overview of PARP Inhibitors for the Treatment of Breast Cancer

(2021) Laura Cortesi et al.   Targeted Oncology

Rapid Detection and Signaling of DNA Damage by PARP-1

(2021) Nootan Pandey et al.   TRENDS IN BIOCHEMICAL SCIENCES

G-quadruplex binding properties of a potent PARP-1 inhibitor derived from 7-azaindole-1-carboxamide

(2021) Sabrina Dallavalle et al.   Scientific Reports

Synchronous conjugation of i-motif DNA and therapeutic siRNA on the vertexes of tetrahedral DNA nanocages for efficient gene silence

(2021) Xiu Han et al.   Acta Pharmaceutica Sinica B

Oncometabolite in Cancer: Current Understanding and Challenges

(2021) Yang Liu et al.   CANCER RESEARCH

Efficacy and mechanism of the combination of PARP and CDK4/6 inhibitors in the treatment of triple-negative breast cancer

(2021) Xiuzhi Zhu et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Breast cancer

(2021) Sibylle Loibl et al.   LANCET

Linking NAD metabolism and DNA repair to inflammation in SSc

(2021) Enrico Vittorio Avvedimento et al.   Nature Reviews Rheumatology

The PARP Enzyme Family and the Hallmarks of Cancer Part 2: Hallmarks Related to Cancer Host Interactions

(2021) Máté A. Demény et al.   Cancers

Novel 4,5-dihydrospiro[benzo[c]azepine-1,1′-cyclohexan]-3(2H)-one derivatives as PARP-1 inhibitors: Design, synthesis and biological evaluation

(2021) Shuai Li et al.   BIOORGANIC CHEMISTRY

Distinct roles for PARP-1 and PARP-2 in c-Myc-driven B-cell lymphoma in mice

(2021) Miguel A Galindo-Campos et al.   BLOOD

PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity

(2021) Joseph M. Gozgit et al.   CANCER CELL

Rationale for combination PARP inhibitor and antiangiogenic treatment in advanced epithelial ovarian cancer: A review

(2021) Angeles Alvarez Secord et al.   GYNECOLOGIC ONCOLOGY

Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP

(2021) Mengzhu Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for Triple-Negative Breast Cancer with Wild-Type BRCA

(2021) Cheng Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Apigenin–Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer

(2021) Huan Long et al.   JOURNAL OF MEDICINAL CHEMISTRY

PARP and CDK4/6 Inhibitor Combination Therapy Induces Apoptosis and Suppresses Neuroendocrine Differentiation in Prostate Cancer

(2021) Cheng Wu et al.   MOLECULAR CANCER THERAPEUTICS

Unsymmetric Cisplatin-Based Pt(IV) Conjugates Containing a PARP-1 Inhibitor Pharmacophore Tested on Malignant Pleural Mesothelioma Cell Lines

(2021) Elisabetta Gabano et al.   MOLECULES

Understanding and overcoming resistance to PARP inhibitors in cancer therapy

(2021) Mariana Paes Dias et al.   Nature Reviews Clinical Oncology

Genetic vulnerabilities upon inhibition of DNA damage response

(2021) Chao Wang et al.   NUCLEIC ACIDS RESEARCH

UPF1 promotes the formation of R loops to stimulate DNA double-strand break repair

(2021) Greg H. P. Ngo et al.   Nature Communications

Serine-linked PARP1 auto-modification controls PARP inhibitor response

(2021) Evgeniia Prokhorova et al.   Nature Communications

Chemical screen identifies shikonin as a broad DNA damage response inhibitor that enhances chemotherapy through inhibiting ATM and ATR

(2021) Fangfang Wang et al.   Acta Pharmaceutica Sinica B

DNA-PK inhibition by M3814 enhances chemosensitivity in non-small cell lung cancer

(2021) Manni Wang et al.   Acta Pharmaceutica Sinica B

Dual PARP and RAD51 Inhibitory Drug Conjugates Show Synergistic and Selective Effects on Breast Cancer Cells

(2021) Matthews M. Malka et al.   Biomolecules

Arsenic compound sensitizes homologous recombination proficient ovarian cancer to PARP inhibitors

(2021) Junfen Xu et al.   Cell Death Discovery

Pamiparib Monotherapy for Patients with Germline BRCA1/2-Mutated Ovarian Cancer Previously Treated with at Least Two Lines of Chemotherapy: A Multicenter, Open-Label, Phase II Study

(2021) Xiaohua Wu et al.   CLINICAL CANCER RESEARCH

Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2

(2021) Jiang Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities

(2021) Xinyue Hu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PARP mediated DNA damage response, genomic stability and immune responses

(2021) Chunyan Zong et al.   INTERNATIONAL JOURNAL OF CANCER

MET inhibition enhances PARP inhibitor efficacy in castration‐resistant prostate cancer by suppressing the ATM/ATR and PI3K/AKT pathways

(2021) Sihai Zhou et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

(2021) Ruben G. G. Leenders et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

(2021) Jeffrey W. Johannes et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Quinazoline-2,4(1H,3H)-dione Derivatives Containing 3-Substituted Piperizines as Potent PARP-1/2 Inhibitors─Design, Synthesis, In Vivo Antitumor Activity, and X-ray Crystal Structure Analysis

(2021) Jie Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

BRD4 orchestrates genome folding to promote neural crest differentiation

(2021) Ricardo Linares-Saldana et al.   NATURE GENETICS

Comparative safety and tolerability of approved PARP inhibitors in cancer: A systematic review and network meta-analysis

(2021) Zhaolun Cai et al.   PHARMACOLOGICAL RESEARCH

Design, synthesis and anticancer activities of novel dual poly(ADP-ribose) polymerase-1/histone deacetylase-1 inhibitors

(2020) Yongbin Tian et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and biological evaluation of erythrina derivatives bearing a 1,2,3-triazole moiety as PARP-1 inhibitors

(2020) Shuai Li et al.   BIOORGANIC CHEMISTRY

EZH2 Inhibition Sensitizes CARM1-High, Homologous Recombination Proficient Ovarian Cancers to PARP Inhibition

(2020) Sergey Karakashev et al.   CANCER CELL

PARP and PARG inhibitors in cancer treatment

(2020) Dea Slade   GENES & DEVELOPMENT

The antitumorigenic roles of BRCA1–BARD1 in DNA repair and replication

(2020) Madalena Tarsounas et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

From PARP1 to TNKS2 Inhibition: A Structure-Based Approach

(2020) Stefano Tomassi et al.   ACS Medicinal Chemistry Letters

Extracellular NAD+ enhances PARP-dependent DNA repair capacity independently of CD73 activity

(2020) Anna Wilk et al.   Scientific Reports

Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2, 3-dioxygenase 1

(2020) Mingxing Hu et al.   Acta Pharmaceutica Sinica B

In vitro and computational studies of natural products related to perezone as anti-neoplastic agents

(2020) Maricarmen Hernández-Rodríguez et al.   BIOCHIMIE

Insights into the functional aspects of poly(ADP‐ribose) polymerase‐1 (PARP‐1) in mitochondrial homeostasis in Dictyostelium discoideum

(2020) Ashlesha Kadam et al.   BIOLOGY OF THE CELL

Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities

(2020) Shanshan Lin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

IDH mutation in glioma: molecular mechanisms and potential therapeutic targets

(2020) Sue Han et al.   BRITISH JOURNAL OF CANCER

Combination of PARP inhibitor olaparib, and PD-L1 inhibitor durvalumab, in recurrent ovarian cancer: a proof-of-concept phase 2 study

(2020) Erika J Lampert et al.   CLINICAL CANCER RESEARCH

BTH-8, a novel poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor, causes DNA double-strand breaks and exhibits anticancer activities in vitro and in vivo

(2020) Chuanlong Guo et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

(2020) Mingzhu Yin et al.   Nature Communications

Identification of Histone deacetylase (HDAC)‐Associated Proteins with DNA‐Programmed Affinity Labeling

(2020) Jianfu Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

First-in-human study of the PARP/tankyrase inhibitor E7449 in patients with advanced solid tumours and evaluation of a novel drug-response predictor

(2020) Ruth Plummer et al.   BRITISH JOURNAL OF CANCER

Combination therapy in advanced urothelial cancer: the role of PARP, HER-2 and mTOR inhibitors

(2020) Veronica Mollica et al.   Expert Review of Anticancer Therapy

PARP inhibitor resistance: the underlying mechanisms and clinical implications

(2020) He Li et al.   Molecular Cancer

Oncometabolites suppress DNA repair by disrupting local chromatin signalling

(2020) Parker L. Sulkowski et al.   NATURE

Machine learning-based genome-wide interrogation of somatic copy number aberrations in circulating tumor DNA for early detection of hepatocellular carcinoma

(2020) Kaishan Tao et al.   EBioMedicine

Design, synthesis, and biological evaluation of quinazolin-4(3H)-one derivatives co-targeting poly(ADP-ribose) polymerase-1 and bromodomain containing protein 4 for breast cancer therapy

(2020) Xiaosa Chang et al.   Acta Pharmaceutica Sinica B

Discovery of Isoquinolinone and Naphthyridinone-based Inhibitors of Poly(ADP-ribose) Polymerase-1 (PARP1) as Anticancer Agents: Structure Activity Relationship and Preclinical Characterization

(2020) Navnath P. Karche et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of 2,3-dihydrobenzo[b][1,4]dioxine-5-carboxamide and 3-oxo-3,4-dihydrobenzo[b][1,4]oxazine-8-carboxamide derivatives as PARP1 inhibitors

(2020) Xuwei Shao et al.   BIOORGANIC CHEMISTRY

AsiDNA Is a Radiosensitizer with no Added Toxicity in Medulloblastoma Pediatric Models

(2020) Sofia Ferreira et al.   CLINICAL CANCER RESEARCH

The ups and downs of Poly(ADP-ribose) Polymerase-1 inhibitors in cancer therapy–Current progress and future direction

(2020) Yue Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Augmentation of the antitumor effects of PARP inhibitors in triple-negative breast cancer via degradation by hydrophobic tagging modulation

(2020) Ahra Go et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers

(2020) Chaoguo Cao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Veliparib with carboplatin and paclitaxel in BRCA-mutated advanced breast cancer (BROCADE3): a randomised, double-blind, placebo-controlled, phase 3 trial

(2020) Véronique Diéras et al.   LANCET ONCOLOGY

BRD4 prevents the accumulation of R-loops and protects against transcription–replication collision events and DNA damage

(2020) Fred C. Lam et al.   Nature Communications

PARP1 inhibitors trigger innate immunity via PARP1 trapping-induced DNA damage response

(2020) Chiho Kim et al.   eLife

Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors

(2020) Hao-Yue Xiang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A very long-acting Poly(ADP-ribose) polymerase inhibitor suppresses cancer cell growth in DNA repair-deficient tumor models

(2020) Shaun D. Fontaine et al.   CANCER RESEARCH

Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer

(2020) Junwei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and evaluation of potential inhibitors for poly(ADP-ribose) polymerase members 1 and 14

(2020) Caleb M Kam et al.   Future Medicinal Chemistry

Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development

(2020) Hexiang Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

NAD+ metabolism and its roles in cellular processes during ageing

(2020) Anthony J. Covarrubias et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The PROTAC technology in drug development

(2019) Yutian Zou et al.   CELL BIOCHEMISTRY AND FUNCTION

Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update

(2019) Priyancy G. Jain et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)

(2019) Carson W. Reed et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploring and comparing adverse events between PARP inhibitors

(2019) Christopher J LaFargue et al.   LANCET ONCOLOGY

Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515

(2019) Gianluca Papeo et al.   ACS Medicinal Chemistry Letters

Updated Efficacy and Safety Data and Impact of the EML4-ALK Fusion Variant on the Efficacy of Alectinib in Untreated ALK-positive Advanced Non-small-cell Lung Cancer in the Global Phase III ALEX Study

(2019) D. Ross Camidge et al.   Journal of Thoracic Oncology

Discovery of Novel Bromophenol–Thiosemicarbazone Hybrids as Potent Selective Inhibitors of Poly(ADP-ribose) Polymerase-1 (PARP-1) for Use in Cancer

(2019) Chuanlong Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

PARP Inhibitors: Extending Benefit Beyond BRCA-Mutant Cancers

(2019) Patrick G. Pilié et al.   CLINICAL CANCER RESEARCH

Design and synthesis of novel PARP-1 inhibitors based on pyridopyridazinone scaffold

(2019) Ghada F. Elmasry et al.   BIOORGANIC CHEMISTRY

Non-NAD-like PARP-1 inhibitors in prostate cancer treatment

(2019) Yaroslava Karpova et al.   BIOCHEMICAL PHARMACOLOGY

Overall survival and updated progression-free survival outcomes in a randomized phase II study of combination cediranib and olaparib versus olaparib in relapsed platinum-sensitive ovarian cancer

(2019) J F Liu et al.   ANNALS OF ONCOLOGY

Discovery of naphthacemycins as a novel class of PARP1 inhibitors

(2019) Wenbin Shen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and Synthesis of Poly(ADP-ribose) Polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-Oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity

(2019) Uday Kiran Velagapudi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Studies Towards Hypoxia-Activated Prodrugs of PARP Inhibitors

(2019) Benjamin D. Dickson et al.   MOLECULES

Discovery of 2-(1-(3-(4-Chloroxyphenyl)-3-oxo- propyl)pyrrolidine-3-yl)-1H-benzo[d]imidazole-4-carboxamide: A Potent Poly(ADP-ribose) Polymerase (PARP) Inhibitor for Treatment of Cancer

(2019) Rui Min et al.   MOLECULES

A decade of clinical development of PARP inhibitors in perspective

(2019) J Mateo et al.   ANNALS OF ONCOLOGY

Design, synthesis and biological evaluation of novel phthalazinone acridine derivatives as dual PARP and Topo inhibitors for potential anticancer agents

(2019) Qiuzi Dai et al.   CHINESE CHEMICAL LETTERS

PARP-1 and its associated nucleases in DNA damage response

(2019) Yijie Wang et al.   DNA REPAIR

Evaluation of absorption, distribution, metabolism, and excretion of [14C]-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors

(2019) Mingxiang Liao et al.   INVESTIGATIONAL NEW DRUGS

Isomerization of BRCA1–BARD1 promotes replication fork protection

(2019) Manuel Daza-Martin et al.   NATURE

Maintenance Olaparib for Germline BRCA-Mutated Metastatic Pancreatic Cancer

(2019) Talia Golan et al.   NEW ENGLAND JOURNAL OF MEDICINE

Small-Molecule Poly(ADP-ribose) Polymerase and PD-L1 Inhibitor Conjugates as Dual-Action Anticancer Agents

(2019) Samuel Ofori et al.   ACS Omega

Combined Strategies with Poly (ADP-Ribose) Polymerase (PARP) Inhibitors for the Treatment of Ovarian Cancer: A Literature Review

(2019) Stergios Boussios et al.   Diagnostics

Radiosensitization of head and neck squamous cell carcinoma lines by DNA-PK inhibitors is more effective than PARP-1 inhibition and is enhanced by SLFN11 and hypoxia

(2019) Tet Woo Lee et al.   INTERNATIONAL JOURNAL OF RADIATION BIOLOGY

Veliparib with First-Line Chemotherapy and as Maintenance Therapy in Ovarian Cancer

(2019) Robert L. Coleman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Design, synthesis and evaluation of phthalazinone thiohydantoin-based derivative as potent PARP-1 inhibitors

(2019) Yi Zhong et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of homoerythrina alkaloid derivatives bearing a triazole moiety as PARP-1 inhibitors and as potential antitumor drugs

(2019) Shuai Li et al.   BIOORGANIC CHEMISTRY

Discovery of novel functionalized 1,2,4-triazoles as PARP-1 inhibitors in breast cancer: Design, synthesis and antitumor activity evaluation

(2019) Ahmed T.A. Boraei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking and Biological Evaluation for Identification of Potential Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors

(2019) Yunjiang Zhou et al.   MOLECULES

Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation

(2019) Shuai Wang et al.   Nature Chemical Biology

PARP Inhibition in Cancer: An Update on Clinical Development

(2019) Esha Sachdev et al.   Targeted Oncology

AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity

(2019) Jacqueline H. L. Fok et al.   Nature Communications

Bone marrow mesenchymal stem cells-derived exosomes for penetrating and targeted chemotherapy of pancreatic cancer

(2019) Yu Zhou et al.   Acta Pharmaceutica Sinica B

Selective phytochemicals targeting pancreatic stellate cells as new anti-fibrotic agents for chronic pancreatitis and pancreatic cancer

(2019) Puvanesswaray Ramakrishnan et al.   Acta Pharmaceutica Sinica B

Crellastatin A, a PARP‐1 Inhibitor Discovered by Complementary Proteomic Approaches

(2019) Elva Morretta et al.   ChemMedChem

Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy

(2019) Junwei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Protein Translation by Rocaglamide and Didesmethylrocaglamide to Treat MPNST and Other Sarcomas

(2019) Long-Sheng Chang et al.   MOLECULAR CANCER THERAPEUTICS

PARP9 enhances infiltration of mononuclear cells in pSS through IFIT1‐mediated upregulation of CXCL10

(2019) Qingqing Tian et al.   Arthritis & Rheumatology

Topoisomerases as anticancer targets

(2018) Justine L. Delgado et al.   BIOCHEMICAL JOURNAL

2,5-Diketopiperazines: A New Class of Poly(ADP-ribose)polymerase Inhibitors

(2018) D. K. Nilov et al.   BIOCHEMISTRY-MOSCOW

Curcumin sensitizes lymphoma cells to DNA damage agents through regulating Rad51-dependent homologous recombination

(2018) Qian Zhao et al.   BIOMEDICINE & PHARMACOTHERAPY

Co-targeting poly(ADP-ribose) polymerase (PARP) and histone deacetylase (HDAC) in triple-negative breast cancer: Higher synergism in BRCA mutated cells

(2018) Hélène Marijon et al.   BIOMEDICINE & PHARMACOTHERAPY

Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer

(2018) Hadia Almahli et al.   BIOORGANIC CHEMISTRY

BRD4 Inhibition Is Synthetic Lethal with PARP Inhibitors through the Induction of Homologous Recombination Deficiency

(2018) Chaoyang Sun et al.   CANCER CELL

Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors

(2018) Xuxing Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PARP inhibitor veliparib and HDAC inhibitor SAHA synergistically co-target the UHRF1/BRCA1 DNA damage repair complex in prostate cancer cells

(2018) Linglong Yin et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Addition of the PARP inhibitor veliparib plus carboplatin or carboplatin alone to standard neoadjuvant chemotherapy in triple-negative breast cancer (BrighTNess): a randomised, phase 3 trial

(2018) Sibylle Loibl et al.   LANCET ONCOLOGY

Krebs-cycle-deficient hereditary cancer syndromes are defined by defects in homologous-recombination DNA repair

(2018) Parker L. Sulkowski et al.   NATURE GENETICS

Characterization of DNA ADP-ribosyltransferase activities of PARP2 and PARP3: new insights into DNA ADP-ribosylation

(2018) Gabriella Zarkovic et al.   NUCLEIC ACIDS RESEARCH

Discovery of quinazoline-2,4(1H,3H)-dione derivatives as novel PARP-1/2 inhibitors: design, synthesis and their antitumor activity

(2018) Jie Zhou et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

NAD+supplementation normalizes key Alzheimer’s features and DNA damage responses in a new AD mouse model with introduced DNA repair deficiency

(2018) Yujun Hou et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Metabolic regulation of transcription through compartmentalized NAD+biosynthesis

(2018) Keun Woo Ryu et al.   SCIENCE

Synthesis and Evaluation of a Mitochondria-Targeting Poly(ADP-ribose) Polymerase-1 Inhibitor

(2018) Tanja Krainz et al.   ACS Chemical Biology

Abstract 4845: Preclinical evaluation of HWH340, a novel PARP inhibitor

(2018) Wenjie Sun et al.   CANCER RESEARCH

Non-canonical Activation of the DNA Sensing Adaptor STING by ATM and IFI16 Mediates NF-κB Signaling after Nuclear DNA Damage

(2018) Gillian Dunphy et al.   MOLECULAR CELL

Talazoparib in Patients with Advanced Breast Cancer and a Germline BRCA Mutation

(2018) Jennifer K. Litton et al.   NEW ENGLAND JOURNAL OF MEDICINE

Synthesis of disaccharide nucleoside analogues as potential poly(ADP-ribose) polymerase-1 inhibitors

(2018) Meng Zheng et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

PARP INHIBITION IN PLATINUM-BASED CHEMOTHERAPY: CHEMOPOTENTIATION AND NEUROPROTECTION

(2018) Rachel M McQuade et al.   PHARMACOLOGICAL RESEARCH

Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors

(2018) Cheng-Zhi Gao et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

BRD4 and Cancer: going beyond transcriptional regulation

(2018) Benedetta Donati et al.   Molecular Cancer

Nuclear cGAS suppresses DNA repair and promotes tumorigenesis

(2018) Haipeng Liu et al.   NATURE

Synthesis and evaluation of an AZD2461 [18F]PET probe in non-human primates reveals the PARP-1 inhibitor to be non-blood-brain barrier penetrant

(2018) Sean W. Reilly et al.   BIOORGANIC CHEMISTRY

Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy

(2017) Wenhua Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy

(2017) Zigao Yuan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 2-substituted 1 H -benzo[ d ]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in vivo anti-tumor activity

(2017) Jie Zhou et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Platinum(IV) prodrugs multiply targeting genomic DNA, histone deacetylases and PARP-1

(2017) Zichen Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Directing the use of DDR kinase inhibitors in cancer treatment

(2017) Inger Brandsma et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Targeting DNA repair and replication stress in the treatment of ovarian cancer

(2017) Junko Murai   International Journal of Clinical Oncology

Rucaparib maintenance treatment for recurrent ovarian carcinoma after response to platinum therapy (ARIEL3): a randomised, double-blind, placebo-controlled, phase 3 trial

(2017) Robert L Coleman et al.   LANCET

Olaparib tablets as maintenance therapy in patients with platinum-sensitive, relapsed ovarian cancer and a BRCA1/2 mutation (SOLO2/ENGOT-Ov21): a double-blind, randomised, placebo-controlled, phase 3 trial

(2017) Eric Pujade-Lauraine et al.   LANCET ONCOLOGY

PARP1 Trapping and DNA Replication Stress Enhance Radiosensitization with Combined WEE1 and PARP Inhibitors

(2017) Leslie A. Parsels et al.   MOLECULAR CANCER RESEARCH

Structure-based design of new poly (ADP-ribose) polymerase (PARP-1) inhibitors

(2017) Navriti Chadha et al.   MOLECULAR DIVERSITY

The multifaceted roles of PARP1 in DNA repair and chromatin remodelling

(2017) Arnab Ray Chaudhuri et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Olaparib for Metastatic Breast Cancer in Patients with a Germline BRCA Mutation

(2017) Mark Robson et al.   NEW ENGLAND JOURNAL OF MEDICINE

CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours

(2017) Hong Xu et al.   Nature Communications

Translational research in radiation-induced DNA damage signaling and repair

(2017) Jac A. Nickoloff et al.   Translational Cancer Research

Poly (ADP-ribose) polymerases inhibitor, Zj6413, as a potential therapeutic agent against breast cancer

(2016) Qin Zhou et al.   BIOCHEMICAL PHARMACOLOGY

Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors

(2016) Junwei Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

NAD + Replenishment Improves Lifespan and Healthspan in Ataxia Telangiectasia Models via Mitophagy and DNA Repair

(2016) Evandro Fei Fang et al.   Cell Metabolism

Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors

(2016) Ann-Gerd Thorsell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer

(2016) Mansoor R. Mirza et al.   NEW ENGLAND JOURNAL OF MEDICINE

Chemical genetic discovery of PARP targets reveals a role for PARP-1 in transcription elongation

(2016) B. A. Gibson et al.   SCIENCE

Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution

(2016) Jin-Xue He et al.   Oncotarget

Crystal structure-based discovery of a novel synthesized PARP1 inhibitor (OL-1) with apoptosis-inducing mechanisms in triple-negative breast cancer

(2016) Leilei Fu et al.   Scientific Reports

Epigenetic polypharmacology: from combination therapy to multitargeted drugs

(2016) Angel R. de Lera et al.   Clinical Epigenetics

The DNA Damage Response: Implications for Tumor Responses to Radiation and Chemotherapy

(2015) Michael Goldstein et al.   Annual Review of Medicine

Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH

(2015) Iskandar Abdullah et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Decitabine priming enhances the antileukemic effects of exportin 1 (XPO1) selective inhibitor selinexor in acute myeloid leukemia

(2015) P. Ranganathan et al.   BLOOD

Hypoxia induced HMGB1 and mitochondrial DNA interactions mediate tumor growth in hepatocellular carcinoma through Toll-like receptor 9

(2015) Yao Liu et al.   JOURNAL OF HEPATOLOGY

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy

(2015) Gianluca Papeo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting the DNA Damage Response in Cancer

(2015) Mark J. O’Connor   MOLECULAR CELL

PARP-1 Activation Requires Local Unfolding of an Autoinhibitory Domain

(2015) Jennine M. Dawicki-McKenna et al.   MOLECULAR CELL

E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling

(2015) Sharon McGonigle 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

Structural basis for the inhibition of poly(ADP-ribose) polymerases 1 and 2 by BMN 673, a potent inhibitor derived from dihydropyridophthalazinone

(2014) Mika Aoyagi-Scharber et al.   Acta Crystallographica Section F-Structural Biology Communications

Olaparib Maintenance Therapy in Platinum-Sensitive Relapsed Ovarian Cancer

(2012) Jonathan Ledermann et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mild hyperthermia inhibits homologous recombination, induces BRCA2 degradation, and sensitizes cancer cells to poly (ADP-ribose) polymerase-1 inhibition

(2011) P. M. Krawczyk et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Crystal Structure of the Catalytic Domain of Human PARP2 in Complex with PARP Inhibitor ABT-888

(2010) Tobias Karlberg et al.   BIOCHEMISTRY

Toward a unified nomenclature for mammalian ADP-ribosyltransferases

(2010) Michael O. Hottiger et al.   TRENDS IN BIOCHEMICAL SCIENCES

The DNA-damage response in human biology and disease

(2009) Stephen P. Jackson et al.   NATURE