PARP inhibitors: polypharmacology versus selective inhibition

A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation

(2013) Ruth Plummer et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

PARP inhibitors in cancer therapy: an update

(2013) Gianluca Papeo et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Tankyrases as drug targets

(2013) Lari Lehtiö et al.   FEBS Journal

Microsatellite instability induced mutations in DNA repair genes CtIP and MRE11 confer hypersensitivity to poly (ADP-ribose) polymerase inhibitors in myeloid malignancies

(2013) T. J. Gaymes et al.   HAEMATOLOGICA

Structural Basis and SAR for G007-LK, a Lead Stage 1,2,4-Triazole Based Specific Tankyrase 1/2 Inhibitor

(2013) Andrew Voronkov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic applications of PARP inhibitors: Anticancer therapy and beyond

(2013) Nicola J. Curtin et al.   MOLECULAR ASPECTS OF MEDICINE

Structural biology of the writers, readers, and erasers in mono- and poly(ADP-ribose) mediated signaling

(2013) Tobias Karlberg et al.   MOLECULAR ASPECTS OF MEDICINE

Poly(ADP-ribose) signaling in cell death

(2013) László Virág et al.   MOLECULAR ASPECTS OF MEDICINE

Identification of Pim Kinases as Novel Targets for PJ34 with Confounding Effects in PARP Biology

(2012) Albert A. Antolín et al.   ACS Chemical Biology

Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939

(2012) Christina A. Kirby et al.   Acta Crystallographica Section F-Structural Biology and Crystallization Communications

Differential anti-proliferative activities of poly(ADP-ribose) polymerase (PARP) inhibitors in triple-negative breast cancer cells

(2012) Hsiao-Ching Chuang et al.   BREAST CANCER RESEARCH AND TREATMENT

Abstract 4688: E7449: A novel PARP inhibitor enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors

(2012) Sharon McGonigle et al.   CANCER RESEARCH

Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors

(2012) J. Murai et al.   CANCER RESEARCH

The Role of PARP-1 and PARP-2 Enzymes in Metabolic Regulation and Disease

(2012) Péter Bai et al.   Cell Metabolism

Failure of Iniparib to Inhibit Poly(ADP-Ribose) Polymerase In Vitro

(2012) A. G. Patel et al.   CLINICAL CANCER RESEARCH

Role of PARP Inhibitors in Cancer Biology and Therapy

(2012) D. Davar et al.   CURRENT MEDICINAL CHEMISTRY

Targeting the DNA damage response in oncology

(2012) Bristi Basu et al.   CURRENT OPINION IN ONCOLOGY

Discovery of Ligands for ADP-Ribosyltransferases via Docking-Based Virtual Screening

(2012) C. David Andersson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Secondary mutations inBRCA2associated with clinical resistance to a PARP inhibitor

(2012) Louise J Barber et al.   JOURNAL OF PATHOLOGY

The DNA damage response and cancer therapy

(2012) Christopher J. Lord et al.   NATURE

Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors

(2012) Elisabet Wahlberg et al.   NATURE BIOTECHNOLOGY

Tankyrase-targeted therapeutics: expanding opportunities in the PARP family

(2012) Jenna L. Riffell et al.   NATURE REVIEWS DRUG DISCOVERY

New insights into the molecular and cellular functions of poly(ADP-ribose) and PARPs

(2012) Bryan A. Gibson et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Unusual increase in lumbar network excitability of the rat spinal cord evoked by the PARP-1 inhibitor PJ-34 through inhibition of glutamate uptake

(2012) Sara Ebrahimi Nasrabady et al.   NEUROPHARMACOLOGY

New readers and interpretations of poly(ADP-ribosyl)ation

(2012) Thomas Kalisch et al.   TRENDS IN BIOCHEMICAL SCIENCES

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

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

Neuroprotective effects of a novel water-soluble poly(ADP-ribose) polymerase-1 inhibitor, MP-124, in in vitro and in vivo models of cerebral ischemia

(2011) Yasuhiro Egi et al.   BRAIN RESEARCH

MP-124, a novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor, ameliorates ischemic brain damage in a non-human primate model

(2011) Shigeru Matsuura et al.   BRAIN RESEARCH

Long-lasting neuroprotection and neurological improvement in stroke models with new, potent and brain permeable inhibitors of poly(ADP-ribose) polymerase

(2011) F Moroni et al.   BRITISH JOURNAL OF PHARMACOLOGY

Iniparib Nonselectively Modifies Cysteine-Containing Proteins in Tumor Cells and Is Not a Bona Fide PARP Inhibitor

(2011) X. Liu et al.   CLINICAL CANCER RESEARCH

PARP-3 and APLF Function Together to Accelerate Nonhomologous End-Joining

(2011) Stuart L. Rulten et al.   MOLECULAR CELL

Re-evaluating PARP1 inhibitor in cancer

(2011) Alexei Tulin   NATURE BIOTECHNOLOGY

PARP inhibitors stumble in breast cancer

(2011) Malini Guha   NATURE BIOTECHNOLOGY

Probing the links between in vitro potency, ADMET and physicochemical parameters

(2011) M. Paul Gleeson et al.   NATURE REVIEWS DRUG DISCOVERY

Poly(ADP-ribose) polymerase 3 (PARP3), a newcomer in cellular response to DNA damage and mitotic progression

(2011) C. Boehler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A snapshot of chemoresistance to PARP inhibitors

(2011) Alberto Chiarugi   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery and characterization of novel potent PARP-1 inhibitors endowed with neuroprotective properties: From TIQ-A to HYDAMTIQ

(2011) Roberto Pellicciari et al.   MedChemComm

A review of PARP inhibitors: from bench to bedside

(2010) C. Underhill et al.   ANNALS OF ONCOLOGY

6-Thioguanine Selectively Kills BRCA2-Defective Tumors and Overcomes PARP Inhibitor Resistance

(2010) N. Issaeva et al.   CANCER RESEARCH

Rational approaches to targeted polypharmacology: creating and navigating protein–ligand interaction networks

(2010) James T Metz et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Drug profiling: knowing where it hits

(2010) Alejandro Merino et al.   DRUG DISCOVERY TODAY

Inhibition of matrix metalloproteinase-2 by PARP inhibitors

(2009) Adrian C. Nicolescu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors

(2009) Danila Branca et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage

(2009) F Moroni et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

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

Structural Basis for Inhibitor Specificity in Human Poly(ADP-ribose) Polymerase-3†

(2009) Lari Lehtiö et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 2-{4-[(3S)-Piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors

(2009) Philip Jones et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

(2009) Shih-Min A. Huang et al.   NATURE

Predicting new molecular targets for known drugs

(2009) Michael J. Keiser et al.   NATURE

Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

(2009) Baozhi Chen et al.   Nature Chemical Biology

Molecular mechanism of poly(ADP-ribosyl)ation by PARP1 and identification of lysine residues as ADP-ribose acceptor sites

(2009) Matthias Altmeyer et al.   NUCLEIC ACIDS RESEARCH

Role of the Peroxynitrite-Poly(ADP-Ribose) Polymerase Pathway in Human Disease

(2008) Pal Pacher et al.   AMERICAN JOURNAL OF PATHOLOGY

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer

(2008) Thomas D. Penning et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phase 0 Trials: An Industry Perspective

(2008) H. Eliopoulos et al.   CLINICAL CANCER RESEARCH

Preclinical Modeling of a Phase 0 Clinical Trial: Qualification of a Pharmacodynamic Assay of Poly (ADP-Ribose) Polymerase in Tumor Biopsies of Mouse Xenografts

(2008) R. J. Kinders et al.   CLINICAL 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

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

A randomized, placebo-controlled trial to evaluate the tolerability, safety, pharmacokinetics, and pharmacodynamics of a potent inhibitor of poly(ADP-ribose) polymerase (INO-1001) in patients with ST-elevation myocardial infarction undergoing primary percutaneous coronary intervention: results of the TIMI 37 trial

(2008) David A. Morrow et al.   JOURNAL OF THROMBOSIS AND THROMBOLYSIS

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

(2008) Wataru Sakai et al.   NATURE

Data completeness—the Achilles heel of drug-target networks

(2008) Jordi Mestres et al.   NATURE BIOTECHNOLOGY

Toward specific functions of poly(ADP-ribose) polymerase-2

(2008) José Yélamos et al.   TRENDS IN MOLECULAR MEDICINE