• 1
    Gibson BA & Kraus WL (2012) New insights into the molecular and cellular functions of poly(ADP-ribose) and PARPs. Nat Rev Mol Cell Biol 13, 411424.
  • 2
    Karlberg T, Langelier MF, Pascal JM & Schüler H (2013) Structural biology of the writers, readers, and erasers in mono- and poly(ADP-ribose) mediated signaling. Mol Aspects Med 34. doi: 10.1016/j.mam.2013.02.002
  • 3
    Kalisch T, Ame JC, Dantzer F & Schreiber V (2012) New readers and interpretations of poly(ADP-ribosyl)ation. Trends Biochem Sci 37, 381390.
  • 4
    Durkacz BW, Omidiji O, Gray DA & Shall S (1980) (ADP-ribose)n participates in DNA excision repair. Nature 283, 593596.
  • 5
    Altmeyer M, Messner S, Hassa PO, Fey M & Hottiger MO (2009) Molecular mechanism of poly(ADP-ribosyl)ation by PARP1 and identification of lysine residues as ADP-ribose acceptor sites. Nucleic Acids Res 37, 37233738.
  • 6
    Lord CJ & Ashworth A (2012) The DNA damage response and cancer therapy. Nature 481, 287294.
  • 7
    Yelamos J, Schreiber V & Dantzer F (2008) Toward specific functions of poly(ADP-ribose) polymerase–2. Trends Mol Med 14, 169178.
  • 8
    Boehler C, Gauthier LR, Mortusewicz O, Biard DS, Saliou JM, Bresson A, Sanglier-Cianferani S, Smith S, Schreiber V, Boussin F et al. (2011) Poly(ADP-ribose) polymerase 3 (PARP3), a newcomer in cellular response to DNA damage and mitotic progression. Proc Natl Acad Sci USA 108, 27832788.
  • 9
    Rulten SL, Fisher AE, Robert I, Zuma MC, Rouleau M, Ju L, Poirier G, Reina-San-Martin B & Caldecott KW (2011) PARP–3 and APLF function together to accelerate nonhomologous end-joining. Mol Cell 41, 3345.
  • 10
    Riffell JL, Lord CJ & Ashworth A (2012) Tankyrase-targeted therapeutics: expanding opportunities in the PARP family. Nat Rev Drug Discov 11, 923936.
  • 11
    Lehtiö L & Krauss S (2013) Tankyrases as drug targets. FEBS J 280, in press. doi: 10.1111/febs.12320.
  • 12
    Plummer R, Jones C, Middleton M, Wilson R, Evans J, Olsen A, Curtin N, Boddy A, McHugh P, Newell D et al. (2008) Phase I study of the poly(ADP-ribose) polymerase inhibitor, AG014699, in combination with temozolomide in patients with advanced solid tumors. Clin Cancer Res 14, 79177923.
  • 13
    Curtin N & Szabo C (2013) Therapeutic applications of PARP inhibitors: anticancer therapy and beyond. Mol Aspects Med 34. doi: 10.1016/j.mam.2013.01.006
  • 14
    Papeo G, Casale E, Montagnoli A & Cirla A (2013) PARP inhibitors in cancer therapy: an update. Expert Opin Ther Pat 23, 503514.
  • 15
    Underhill C, Toulmonde M & Bonnefoi H (2011) A review of PARP inhibitors: from bench to bedside. Ann Oncol 22, 268279.
  • 16
    Bryant HE, Schultz N, Thomas HD, Parker KM, Flower D, Lopez E, Kyle S, Meuth M, Curtin NJ & Helleday T (2005) Specific killing of BRCA2-deficient tumours with inhibitors of poly(ADP-ribose) polymerase. Nature 434, 913917.
  • 17
    Farmer H, McCabe N, Lord CJ, Tutt AN, Johnson DA, Richardson TB, Santarosa M, Dillon KJ, Hickson I, Knights C et al. (2005) Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature 434, 917921.
  • 18
    Basu B, Yap TA, Molife LR & de Bono JS (2012) Targeting the DNA damage response in oncology: past, present and future perspectives. Curr Opin Oncol 24, 316324.
  • 19
    Cosi C, Suzuki H, Milani D, Facci L, Menegazzi M, Vantini G, Kanai Y & Skaper SD (1994) Poly(ADP-ribose) polymerase: early involvement in glutamate-induced neurotoxicity in cultured cerebellar granule cells. J Neurosci Res 39, 3846.
  • 20
    Love S, Barber R & Wilcock GK (1999) Neuronal accumulation of poly(ADP-ribose) after brain ischaemia. Neuropathol Appl Neurobiol 25, 98103.
  • 21
    Moroni F, Formentini L, Gerace E, Camaioni E, Pellegrini-Giampietro DE, Chiarugi A & Pellicciari R (2009) Selective PARP–2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Br J Pharmacol 157, 854862.
  • 22
    Virag L, Robaszkiewicz A, Rodriguez-Vargas JM & Oliver FJ (2013) Poly(ADP-ribose) signaling in cell death. Mol Aspects Med 34. doi: 10.1016/j.mam.2013.01.007
  • 23
    Eliasson MJ, Sampei K, Mandir AS, Hurn PD, Traystman RJ, Bao J, Pieper A, Wang ZQ, Dawson TM, Snyder SH et al. (1997) Poly(ADP-ribose) polymerase gene disruption renders mice resistant to cerebral ischemia. Nat Med 3, 10891095.
  • 24
    Endres M, Wang ZQ, Namura S, Waeber C & Moskowitz MA (1997) Ischemic brain injury is mediated by the activation of poly(ADP-ribose)polymerase. J Cereb Blood Flow Metab 17, 11431151.
  • 25
    Moroni F, Cozzi A, Chiarugi A, Formentini L, Camaioni E, Pellegrini-Giampietro DE, Chen Y, Liang S, Zaleska MM, Gonzales C et al. (2012) Long-lasting neuroprotection and neurological improvement in stroke models with new, potent and brain permeable inhibitors of poly(ADP-ribose) polymerase. Br J Pharmacol 165, 14871500.
  • 26
    Pacher P & Szabo C (2008) Role of the peroxynitrite-poly(ADP-ribose) polymerase pathway in human disease. Am J Pathol 173, 213.
  • 27
    Molnar A, Toth A, Bagi Z, Papp Z, Edes I, Vaszily M, Galajda Z, Papp JG, Varro A, Szuts V et al. (2006) Activation of the poly(ADP-ribose) polymerase pathway in human heart failure. Mol Med 12, 143152.
  • 28
    Matsuura S, Egi Y, Yuki S, Horikawa T, Satoh H & Akira T (2011) MP–124, a novel poly(ADP-ribose) polymerase–1 (PARP–1) inhibitor, ameliorates ischemic brain damage in a non-human primate model. Brain Res 1410, 122131.
  • 29
    Egi Y, Matsuura S, Maruyama T, Fujio M, Yuki S & Akira T (2011) 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. Brain Res 1389, 169176.
  • 30
    Pellicciari R, Camaioni E, Gilbert AM, Macchiarulo A, Bikker JA, Shah F, Bard J, Costantino G, Gioiello A, Robertson GM et al. (2011) Discovery and characterization of novel potent PARP–1 inhibitors endowed with neuroprotective properties: from TIQ–A to HYDAMTIQ. Med Chem Comm 2, 559565.
  • 31
    Morrow DA, Brickman CM, Murphy SA, Baran K, Krakover R, Dauerman H, Kumar S, Slomowitz N, Grip L, McCabe CH et al. (2009) 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. J Thromb Thrombolysis 27, 359364.
  • 32
    Bai P & Canto C (2012) The role of PARP–1 and PARP–2 enzymes in metabolic regulation and disease. Cell Metab 16, 290295.
  • 33
    Dölle C, Rack & Ziegler M (2013) NAD+ADPR metabolism in mito. FEBS J 280.
  • 34
    Thomas HD, Calabrese CR, Batey MA, Canan S, Hostomsky Z, Kyle S, Maegley KA, Newell DR, Skalitzky D, Wang LZ et al. (2007) Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther 6, 945956.
  • 35
    Plummer R, Lorigan P, Steven N, Scott L, Middleton MR, Wilson RH, Mulligan E, Curtin N, Wang D, Dewji R et al. (2013) A phase II study of the potent PARP inhibitor, Rucaparib (PF–01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation. Cancer Chemother Pharmacol 71, 11911199.
  • 36
    Jagtap P, Soriano FG, Virág L, Liaudet L, Mabley J, Szabó E, Haskó G, Marton A, Lorigados CB, Gallyas F Jr et al. (2002) Novel phenanthridinone inhibitors of poly (adenosine 5′–diphosphate-ribose) synthetase: potent cytoprotective and antishock agents. Crit Care Med 30, 10711082.
  • 37
    Jagtap PG, Baloglu E, Southan GJ, Mabley JG, Li H, Zhou J, van Duzer J, Salzman AL & Szabó C (2005) Discovery of potent poly(ADP-ribose) polymerase–1 inhibitors from the modification of indeno[1,2–c]isoquinolinone. J Med Chem 48, 51005103.
  • 38
    Bedikian AY, Papadopoulos NE, Kim KB, Hwu WJ, Homsi J, Glass MR, Cain S, Rudewicz P, Vernillet L & Hwu P (2009) A phase IB trial of intravenous INO–1001 plus oral temozolomide in subjects with unresectable stage-III or IV melanoma. Cancer Invest 27, 756763.
  • 39
    Zhang J (1999) PARP inhibition: a novel approach to treat ischaemia/reperfusion and inflammation-related injuries. Expert Opin Emerg Drugs 4, 209221.
  • 40
    Lapidus RG, Xu W, Spicer E, Hoover R & Zhang J (2006) PARP inhibitors enhance the effect of cisplatin against tumors and ameliorate cisplatin-induced neuropathy. Presented at the 97th Annual Meeting of the American Association for Cancer Research, American Association for Cancer Research, Washington DC.
  • 41
    Russo AL, Kwon HC, Burgan WE, Carter D, Beam K, Weizheng X, Zhang J, Slusher BS, Chakravarti A, Tofilon PJ et al. (2009) In vitro and in vivo radiosensitization of glioblastoma cells by the poly (ADP-ribose) polymerase inhibitor E7016. Clin Cancer Res 15, 607612.
  • 42
    McGonigle S, Chen Z, Wu J, Ackermann K, Tendyke K, Moniz G & Nomato K (2012) E7449: a novel PARP inhibitor enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors. Cancer Res 72, doi: 10.1158/1538-7445.AM2012-4688.
  • 43
    Ator MA, Bihovsky R, Chatterjee S, Dunn D & Hudkins RL (2001) WO–200185686/US-2002028815
  • 44
    Tao M, Park CH, Bihovsky R, Wells GJ, Husten J, Ator MA & Hudkins RL (2006) Synthesis and structure–activity relationships of novel poly(ADP-ribose) polymerase–1 inhibitors. Bioorg Med Chem Lett 16, 938942.
  • 45
    Miknyoczki S, Chang H, Grobelny J, Pritchard S, Worrell C, McGann N, Ator M, Husten J, Deibold J, Hudkins R et al. (2007) The selective poly(ADP-ribose) polymerase–1(2) inhibitor, CEP–8983, increases the sensitivity of chemoresistant tumor cells to temozolomide and irinotecan but does not potentiate myelotoxicity. Mol Cancer Ther 6, 22902302.
  • 46
    Shen Y, Feng Y, Wang B, Myers P, Chu D & Post LE (2011) Structure and preclinical characterization of BMN 673, a potent and orally active PARP inhibitor as an anticancer agent. Mol Cancer Ther 10(Suppl. 1), abstract B64.
  • 47
    Gaymes TJ, Mohamedali AM, Patterson M, Matto N, Smith A, Kulasekararaj A, Chelliah R, Curtin N, Farzaneh F, Shall S et al. (2013) Microsatellite instability induced mutations in DNA repair genes Ctip and MRE11 confer hypersensitivity to poly (ADP-ribose) polymerase (PARP) inhibitors in myeloidmalignancies. Haematologica, doi: 10.3324/haematol.2012.079251.
  • 48
    Davar D, Beumer JH, Hamieh L & Tawbi H (2012) Role of PARP inhibitors in cancer biology and therapy. Curr Med Chem 19, 39073921.
  • 49
    Branca D, Cerretani M, Jones P, Koch U, Orvieto F, Palumbi MC, Rowley M, Toniatti C & Muraglia E (2009) Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase–1 inhibitors. Bioorg Med Chem Lett 19, 40424045.
  • 50
    Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV et al. (2009) 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. J Med Chem 52, 71707185.
  • 51
    Bhargava S, Mueller S, Wehmeijer L, Yang X, Gragg A, Matthay KK, Weiss WA & Haas-Kogan DA (2011) PARP–1 inhibitor MK–4827 in combination with radiation as a treatment strategy for metastatic neuroblastoma. J Clin Oncol 29(Suppl.), abstract 9559.
  • 52
    Donawho CK, Luo Y, Luo Y, Penning TD, Bauch JL, Bouska JJ, Bontcheva-Diaz VD, Cox BF, DeWeese TL, Dillehay LE et al. (2007) ABT–888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res 13, 27282737.
  • 53
    Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH et al. (2008) 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. Bioorg Med Chem 16, 69656975.
  • 54
    Kinders RJ, Hollingshead M, Khin S, Rubinstein L, Tomaszewski JE, Doroshow JH, Parchment RE & the National Cancer Institute Phase 0 Clinical Trials Team (2008) Preclinical modeling of a phase 0 clinical trial: qualification of a pharmacodynamic assay of poly (ADP-ribose) polymerase in tumor biopsies of mouse xenografts. Clin Cancer Res 14, 68776885.
  • 55
    Eliopoulos H, Giranda V, Carr R, Tiehen R, Leahy T & Gordon G (2008) Phase 0 trials: an industry perspective. Clin Cancer Res 14, 36833688.
  • 56
    Isakoff SJ, Overmoyer B, Tung NM, Gelman RS, Giranda VL, Bernhard KM, Habin KR, Ellisen LW, Winer EP & Goss PE (2010) A phase II trial of the PARP inhibitor veliparib (ABT888) and temozolomide for metastatic breast cancer. J Clin Oncol 28(Suppl.), abstract 1019.
  • 57
    Loh VM Jr, Cockcroft XL, Dillon KJ, Dixon L, Drzewiecki J, Eversley PJ, Gomez S, Hoare J, Kerrigan F, Matthews IT et al. (2005) Phthalazinones. Part 1: the design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase. Bioorg Med Chem Lett 15, 22352238.
  • 58
    Cockcroft XL, Dillon KJ, Dixon L, Drzewiecki J, Kerrigan F, Loh VM Jr, Martin NM, Menear KA & Smith GC (2006) Phthalazinones 2: optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase. Bioorg Med Chem Lett 16, 10401044.
  • 59
    Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S et al. (2008) 4–[3–(4–cyclopropanecarbonylpiperazine-1–carbonyl)-4–fluorobenzyl]-2H–phthalazin-1–one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase–1. J Med Chem 51, 65816591.
  • 60
    Chiarugi A (2012) A snapshot of chemoresistance to PARP inhibitors. Trends Pharmacol Sci 33, 4248.
  • 61
    Sakai W, Swisher EM, Karlan BY, Agarwal MK, Higgins J, Friedman C, Villegas E, Jacquemont C, Farrugia DJ, Couch FJ et al. (2008) Secondary mutations as a mechanism of cisplatin resistance in BRCA2-mutated cancers. Nature 451, 11161120.
  • 62
    Barber LJ, Sandhu S, Chen L, Campbell J, Kozarewa I, Fenwick K, Assiotis I, Rodrigues DN, Filho JS, Moreno V et al. (2013) Secondary mutations in BRCA2 associated with clinical resistance to a PARP inhibitor. J Pathol 229, 422429.
  • 63
    Issaeva N, Thomas HD, Djureinovic T, Jaspers JE, Stoimenov I, Kyle S, Pedley N, Gottipati P, Zur R, Sleeth K et al. (2010) 6–Thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res 70, 62686276.
  • 64
    Jaspers JE, Kersbergen A, Boon U, Sol W, van Deemter L, Zander SA, Drost R, Wientjens E, Ji J, Aly A et al. (2013) Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov 3, 6881.
  • 65
    Buki KG, Bauer PI, Mendeleyev J, Hakam A & Kun E (1991) Destabilization of Zn2+ coordination in ADP-ribose transferase (polymerizing) by 6–nitroso-1,2–benzopyrone coincidental with inactivation of the polymerase but not the DNA binding function. FEBS Lett 290, 181185.
  • 66
    Tseng A Jr, Lee WM, Jakobovits EB, Kirsten E, Hakam A, McLick J, Buki K & Kun E (1987) Prevention of tumorigenesis of oncogene-transformed rat fibroblasts with DNA site inhibitors of poly(ADP ribose) polymerase. Proc Natl Acad Sci USA 84, 11071111.
  • 67
    Kun E, Mendeleyev J, Basbaurn C, Lemjabbar-alaoui H & Ossovskaya V (2007) WO-2007011962/US-2007015837
  • 68
    Patel AG, De Lorenzo SB, Flatten KS, Poirier GG & Kaufmann SH (2012) Failure of iniparib to inhibit poly(ADP-ribose) polymerase in vitro. Clin Cancer Res 18, 16551662.
  • 69
    Liu X, Shi Y, Maag DX, Palma JP, Patterson MJ, Ellis PA, Surber BW, Ready DB, Soni NB, Ladror US et al. (2012) Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res 18, 510523.
  • 70
    Guha M (2011) PARP inhibitors stumble in breast cancer. Nat Biotechnol 29, 373374.
  • 71
    Tulin A (2011) Re-evaluating PARP1 inhibitor in cancer. Nat Biotechnol 29, 10781079.
  • 72
    Murai J, Huang SY, Das BB, Renaud A, Zhang Y, Doroshow JH, Ji J, Takeda S & Pommier Y (2012) Trapping of PARP1 and PARP2 by clinical PARP inhibitors. Cancer Res 72, 55885599.
  • 73
    Chuang HC, Kapuriya N, Kulp SK, Chen CS & Shapiro CL (2012) Differential anti-proliferative activities of poly(ADP-ribose) polymerase (PARP) inhibitors in triple-negative breast cancer cells. Breast Cancer Res Treat 134, 649659.
  • 74
    Merino A, Bronowska AK, Jackson DB & Cahill DJ (2010) Drug profiling: knowing where it hits. Drug Discov Today 15, 749756.
  • 75
    Metz JT & Hajduk PJ (2010) Rational approaches to targeted polypharmacology: creating and navigating protein–ligand interaction networks. Curr Opin Chem Biol 14, 498504.
  • 76
    Keiser MJ, Setola V, Irwin JJ, Laggner C, Abbas AI, Hufeisen SJ, Jensen NH, Kuijer MB, Matos RC, Tran TB et al. (2009) Predicting new molecular targets for known drugs. Nature 462, 175181.
  • 77
    Oprea TI, Tropsha A, Faulon JL & Rintoul MD (2007) Systems chemical biology. Nat Chem Biol 3, 447450.
  • 78
    Keiser MJ, Roth BL, Armbruster BN, Ernsberger P, Irwin JJ & Shoichet BK (2007) Relating protein pharmacology by ligand chemistry. Nat Biotechnol 25, 197206.
  • 79
    Paolini GV, Shapland RH, van Hoorn WP, Mason JS & Hopkins AL (2006) Global mapping of pharmacological space. Nat Biotechnol 24, 805815.
  • 80
    Gleeson MP, Hersey A, Montanari D & Overington J (2011) Probing the links between in vitro potency, ADMET and physicochemical parameters. Nat Rev Drug Discov 10, 197208.
  • 81
    Mestres J, Gregori-Puigjane E, Valverde S & Sole RV (2008) Data completeness – the Achilles heel of drug–target networks. Nat Biotechnol 26, 983984.
  • 82
    Wahlberg E, Karlberg T, Kouznetsova E, Markova N, Macchiarulo A, Thorsell AG, Pol E, Frostell Å, Ekblad T, Öncü D et al. (2012) Family wide chemical profiling and structural analysis of PARP and tankyrase inhibitors. Nat Biotechnol 30, 283288.
  • 83
    Hopkins AL, Mason JS & Overington JP (2006) Can we rationally design promiscuous drugs? Curr Opin Struct Biol 16, 127136.
  • 84
    Morphy R & Rankovic Z (2007) Fragments, network biology and designing multiple ligands. Drug Discov Today 12, 156160.
  • 85
    Antolin AA, Jalencas X, Yelamos J & Mestres J (2012) Identification of Pim kinases as novel targets for PJ34 with confounding effects in PARP biology. ACS Chem Biol 7, 19621967.
  • 86
    Nicolescu AC, Holt A, Kandasamy AD, Pacher P & Schulz R (2009) Inhibition of matrix metalloproteinase–2 by PARP inhibitors. Biochem Biophys Res Commun 387, 646650.
  • 87
    Nasrabady SE, Kuzhandaivel A, Akrami A, Bianchetti E, Milanese M, Bonanno G & Nistri A (2012) Unusual increase in lumbar network excitability of the rat spinal cord evoked by the PARP–1 inhibitor PJ–34 through inhibition of glutamate uptake. Neuropharmacology 63, 415426.
  • 88
    Kirby CA, Cheung A, Fazal A, Shultz MD & Stams T (2012) Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939. Acta Crystallogr Sect F Struct Biol Cryst Commun 68, 115118.
  • 89
    Lehtio L, Jemth AS, Collins R, Loseva O, Johansson A, Markova N, Hammarstrom M, Flores A, Holmberg-Schiavone L, Weigelt J et al. (2009) Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase–3. J Med Chem 52, 31083111.
  • 90
    Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS et al. (2009) Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol 5, 100107.
  • 91
    Huang SM, Mishina YM, Liu S, Cheung A, Stegmeier F, Michaud GA, Charlat O, Wiellette E, Zhang Y, Wiessner S et al. (2009) Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461, 614620.
  • 92
    Voronkov A, Holsworth DD, Waaler J, Wilson SR, Ekblad B, Perdreau-Dahl H, Dinh H, Drewes G, Hopf C, Morth JP et al. (2013) Structural basis and SAR for G007–LK, a lead stage 1,2,4–triazole based specific tankyrase 1/2 inhibitor. J Med Chem 56, 30123023.
  • 93
    Andersson CD, Karlberg T, Ekblad T, Lindgren AE, Thorsell AG, Spjut S, Uciechowska U, Niemiec MS, Wittung-Stafshede P, Weigelt J et al. (2012) Discovery of ligands for ADP-ribosyltransferases via docking-based virtual screening. J Med Chem 55, 77067718.