Polo-like kinase 1 inhibitors in mono- and combination therapies: a new strategy for treating malignancies

References

• Yap TA, Molife LR, Blagden SP et al. Targeting cell cycle kinases and kinesins in anticancer drug development. Expert Opin. Drug Discov.2(4), 539–560 (2007).
   PubMed Web of Science ®Google Scholar
• Liu X, Erikson RL. Polo-like kinase (Plk)1 depletion induces apoptosis in cancer cells. Proc. Natl Acad. Sci. USA100(10), 5789–5794 (2003).
   PubMed Web of Science ®Google Scholar
• Eckerdt F, Yuan J, Strebhardt K. Polo-like kinases and oncogenesis. Oncogene24(2), 267–276 (2005).
   PubMed Web of Science ®Google Scholar
• Strebhardt K. Multifaceted Polo-like kinases: drug targets and antitargets for cancer therapy. Nat. Rev. Drug Discov.9(8), 643–660 (2010).
   PubMed Web of Science ®Google Scholar
• Petronczki M, Lenart P, Peters JM. Polo on the rise – from mitotic entry to cytokinesis with PLK1. Dev. Cell14(5), 646–659 (2008).
   PubMed Web of Science ®Google Scholar
• Johnson EF, Stewart KD, Woods KW et al. Pharmacological and functional comparison of the Polo-like kinase family: insight into inhibitor and substrate specificity. Biochemistry46(33), 9551–9563 (2007).
   PubMed Web of Science ®Google Scholar
• Strebhardt K, Ullrich A. Targeting Polo-like kinase 1 for cancer therapy. Nat. Rev. Cancer6(4), 321–330 (2006).
   PubMed Web of Science ®Google Scholar
• Andrysik Z, Bernstein WZ, Deng L et al. The novel mouse Polo-like kinase 5 responds to DNA damage and localizes in the nucleolus. Nucleic Acids Res.38(9), 2931–2943 (2010).
   PubMed Web of Science ®Google Scholar
• Reindl W, Yuan J, Kramer A et al. Inhibition of Polo-like kinase 1 by blocking Polo-box domain-dependent protein–protein interactions. Chem. Biol.15(5), 459–466 (2008).
   PubMed Web of Science ®Google Scholar
• McInnes C, Mezna M, Fischer PM. Progress in the discovery of Polo-like kinase inhibitors. Curr. Top. Med. Chem.5(2), 181–197 (2005).
   PubMed Web of Science ®Google Scholar
• Barr FA, Sillje HHW, Nigg EA. Polo-like kinases and the orchestration of cell division. Nat. Rev. Mol. Cell. Biol.5(6), 429–440 (2004).
   PubMed Web of Science ®Google Scholar
• Takaki T, Trenz K, Costanzo V et al. Polo-like kinase 1 reaches beyond mitosis – cytokinesis, DNA damage response, and development. Curr. Opin. Cell Biol.20(6), 650–660 (2008).
   PubMed Web of Science ®Google Scholar
• Uckun FM, Ozer Z, Qazi S et al. Polo-like-kinase 1 (PLK1) as a molecular target to overcome SYK-mediated resistance of B-lineage acute lymphoblastic leukaemia cells to oxidative stress. Br. J. Haematol.148(5), 714–725 (2010).
   PubMedGoogle Scholar
• Renner AG, Dos Santos C, Recher C et al. Polo-like kinase 1 is overexpressed in acute myeloid leukemia and its inhibition preferentially targets the proliferation of leukemic cells. Blood114(3), 659–662 (2009).
   PubMed Web of Science ®Google Scholar
• Plyte S, Musacchio A. PLK1 inhibitors: setting the mitotic death trap. Curr. Biol.17(8), R280–R283 (2007).
   PubMedGoogle Scholar
• Stevenson CS, Capper EA, Roshak AK et al. Scytonemin – a marine natural product inhibitor of kinases key in hyperproliferative inflammatory diseases. Inflamm. Res.51(2), 112–114 (2002).
   PubMed Web of Science ®Google Scholar
• Stevenson CS, Capper EA, Roshak AK et al. The identification and characterization of the marine natural product scytonemin as a novel antiproliferative pharmacophore. J. Pharmacol. Exp. Ther.303(2), 858–866 (2002).
   PubMed Web of Science ®Google Scholar
• Amado RG, Wolf M, Peeters M et al. Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer. J. Clin. Oncol.26(10), 1626–1634 (2008).
   PubMed Web of Science ®Google Scholar
• Kothe M, Kohls D, Low S et al. Structure of the catalytic domain of human Polo-like kinase 1. Biochemistry46(20), 5960–5971 (2007).
   PubMed Web of Science ®Google Scholar
• Steegmaier M, Hoffmann M, Baum A et al. BI 2536, a potent and selective inhibitor of Polo-like kinase 1, inhibits tumor growth in vivo. Curr. Biol.17(4), 316–322 (2007).
   PubMed Web of Science ®Google Scholar
• Lenart P, Petronczki M, Steegmaier M et al. The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of Polo-like kinase 1. Curr. Biol.17(4), 304–315 (2007).
   PubMed Web of Science ®Google Scholar
• Mross K, Frost A, Steinbild S et al. Phase I dose escalation and pharmacokinetic study of BI 2536, a novel Polo-like kinase 1 inhibitor, in patients with advanced solid tumors. J. Clin. Oncol.26(34), 5511–5517 (2008).
   PubMed Web of Science ®Google Scholar
• Vose JM, Young A, Friedberg JW et al. Phase I dose-escalation trial of BI 2536, a Polo-like kinase 1 inhibitor, in relapsed and refractory non-Hodgkin’s lymphoma [abstract]. BloodASH Ann. Meeting Abstr.112(11), 233 (2008).
   Google Scholar
• Müller-Tidow C, Bug G, Schlenk R et al. Phase I/II study of BI 2536, an intravenous Polo-like kinase-1 (Plk-1) inhibitor, in elderly patients with relapsed or refractory acute myeloid leukemia (AML): first results of a multi-center trial [abstract]. BloodASH Ann. Meeting Abstr.112(11), 2973 (2008).
   PubMedGoogle Scholar
• Munzert G, Steinbild S, Frost A et al. A Phase I study of two administration schedules of the Polo-like kinase 1 inhibitor BI 2536 in patients with advanced solid tumors [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc.24(18 Suppl.), 3069 (2006).
   PubMed Web of Science ®Google Scholar
• Hofheinz R, Hochhaus A, Al-Batran S et al. A Phase I repeated dose escalation study of the Polo-like kinase 1 inhibitor BI 2536 in patients with advanced solid tumours [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc. Part I24(18 Suppl.), 2038 (2006).
   PubMed Web of Science ®Google Scholar
• Ellis PM, Chu QS, Leighl NB et al. A Phase I dose escalation trial of BI 2536, a novel Plk1 inhibitor, with standard dose pemetrexed in previously treated advanced or metastatic non-small cell lung cancer (NSCLC) [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc.26(15 Suppl.), 8115 (2008).
   Google Scholar
• Sebastian M, Reck M, Waller CF et al. The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized Phase II clinical trial. J. Thorac. Oncol.5(7), 1060–1067 (2010).
   PubMed Web of Science ®Google Scholar
• Mross K, Dittrich C, Aulitzky WE et al. A randomized Phase II trial of the novel Polo-like kinase 1 inhibitor BI 2536 in chemonaïve patients with unresectable advanced pancreatic cancer – a study in cooperation with the CESAR network of investigators [abstract]. Ann. Oncol.19(8), viii153 (2008).
   Google Scholar
• Gandhi L, Chu QS, Stephenson J et al. An open label Phase II trial of the Plk1 inhibitor BI 2536, in patients with sensitive relapse small cell lung cancer (SCLC) [abstract]. J. Clin. Oncol. ASCO Ann. Meeting Abstract Proc.27(15 Suppl.), 8108 (2009).
   Google Scholar
• Schöffski P, Blay JY, De Greve J et al. Multicentric parallel Phase II trial of the Polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research and Treatment of Cancer (EORTC) Network Of Core Institutes (NOCI). Eur. J. Cancer46(12), 2206–2215 (2010).
   PubMed Web of Science ®Google Scholar
• Rudolph D, Steegmaier M, Hoffmann M et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin. Cancer Res.15(9), 3094–3102 (2009).
   PubMed Web of Science ®Google Scholar
• Schöffski P, Awad L, Dumez H et al. A Phase I single dose escalation study of the novel Polo-like kinase 1 inhibitor BI 6727 in patients with advanced solid tumours [abstract]. Eur. J. Cancer Suppl.6(12), 14–15 (2008).
   Google Scholar
• Stadler WM, Cao D, Vogelzang NJ et al. A randomized Phase II trial of the antiangiogenic agent SU5416 in hormone-refractory prostate cancer. Clin. Cancer Res.10(10), 3365–3370 (2004).
   PubMed Web of Science ®Google Scholar
• Laquerre S, Sung C-M, Gilmartin A et al. A potent and selective Polo-like kinase 1 (Plk1) Inhibitor (GSK461364) induces cell cycle arrest and growth inhibition of cancer cell [abstract]. Proceedings of: The 98th Annual Meeting of the AACR. Philadelphia, PA, USA, 13–17 April 2007 (Abstract 5389).
   Google Scholar
• Ikezoe T, Yang J, Nishioka C et al. A novel treatment strategy targeting Polo-like kinase 1 in hematological malignancies. Leukemia23(9), 1564–1576 (2009).
   PubMed Web of Science ®Google Scholar
• Olmos D, Barker D, Sharma R et al. Phase I study of GSK461364, a specific and competitive Polo-like kinase 1 (Plk1) inhibitor in patients with advanced solid malignancies. Clin. Cancer Res.17(10), 3420–3430 (2011).
   PubMed Web of Science ®Google Scholar
• Didier C, Cavelier C, Quaranta M et al. Evaluation of Polo-like kinase 1 inhibition on the G2/M checkpoit in acute myelocytic leukemia. Eur. J. Pharmacol.591(1–3), 102–105 (2008).
   PubMed Web of Science ®Google Scholar
• Gumireddy K, Reddy MV, Cosenza SC et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell7(3), 275–286 (2005).
   PubMed Web of Science ®Google Scholar
• Donehower RC, Jimeno A, Li J et al. Phase I study of ON-01910.Na, a novel cell cycle inhibitor in adult patients with solid tumors [abstract]. In J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc. Part I24(18 Suppl.), 13026 (2006).
   Google Scholar
• Ghalib M, Weinstein J, Maniar M et al. ON01910.Na, a novel Polo-like kinase pathway modulator as a treatment for patients with advanced cancer [abstract]. Proceedings of: The 99th Annual Meeting of the AACR. Washington, DC, USA, 12–16 April 2008 (Abstract 5652).
   Google Scholar
• Ohnuma T, Cho SY, Roboz J et al. Phase I study of ON 01910.Na by 3-day continuous infusion (CI) in patients (pts) with advanced cancer [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc. Part I24(18 Suppl.), 13137 (2006).
   Google Scholar
• Vainshtein JM, Ghalib MH, Kumar M et al. Phase I study of ON 01910.Na, a novel Polo-like kinase 1 pathway modulator, administered as a weekly 24-hour continuous infusion in patients with advanced cancer [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc.26(15 Suppl.), 2515 (2008).
   Google Scholar
• Jimeno A, Li J, Messersmith WA et al. Phase I study of ON 01910.Na, a novel modulator of the Polo-like kinase 1 pathway, in adult patients with solid tumors. J. Clin. Oncol.26(34), 5504–5510 (2008).
   PubMed Web of Science ®Google Scholar
• Chapman C, Perez-Galan P, Wiestner A. Na, a novel clinical grade PLK-1 inhibitor, selectively induces apoptosis in human B-cell chronic lymphocytic leukemia (B-CLL) [abstract]. Proceedings of: The 100th Annual Meeting of the AACR. Denver, CO, USA, 18–22 April 2009 (Abstract 3654).
   Google Scholar
• Garland LL, Taylor C, Pilkington DL et al. A Phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with Polo-like kinase-1-interacting properties, in patients with advanced solid tumors. Clin. Cancer Res.12(17), 5182–5189 (2006).
   PubMed Web of Science ®Google Scholar
• Takagi M, Honmura T, Watanabe S et al. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest. New Drugs21(4), 387–399 (2003).
   PubMed Web of Science ®Google Scholar
• Tanaka H, Ohshima N, Ikenoya M et al. HMN-176, an active metabolite of the synthetic antitumor agent HMN-214, restores chemosensitivity to multidrug-resistant cells by targeting the transcription factor NF-Y. Cancer Res.63(20), 6942–6947 (2003).
   PubMed Web of Science ®Google Scholar
• Patnaik A, Forero L, Goetz A et al. HMN-214, a novel oral antimicrotubular agent and inhibitor of Polo-like- and cyclin-dependent kinases: clinical, pharmacokinetic (PK) and pharmacodynamic (PD) relationships observed in a Phase I trial of a daily × 5 schedule every 28 days [abstract]. Proc. Am. Soc. Clin. Oncol.22, 514 (2003).
   Google Scholar
• Von Hoff DD, Taylor C, Rubin S et al. A Phase I and pharmacokinetic study of HMN-214, a novel oral Polo-like kinase inhibitor, in patients with advanced solid tumors [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc.22(14 Suppl.), 3034 (2004).
   Google Scholar
• Beria I, Ballinari D, Bertrand JA et al. Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. J. Med. Chem.53(9), 3532–3551 (2010).
   PubMed Web of Science ®Google Scholar
• Beria I, Bossi RT, Brasca MG et al. NMS-P937, a 4,5 -dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg. Med. Chem. Lett. (2011) (In Press).
   Google Scholar
• Valsasina B, Beria I, Alzani R et al. Pyrazoloquinazolines: From an unselective hit to a potent Plk-1 specific inhibitor. Proceedings of: The 100th Annual meeting of the AACR. Denver, CO, USA, 18–22 April 2009 (Abstract 1812).
   Google Scholar
• Sato Y, Onozaki Y, Sugimoto T et al. Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors. Bioorg. Med. Chem. Lett19(16), 4673–4678 (2009).
   PubMed Web of Science ®Google Scholar
• Peters U, Cherian J, Kim JH et al. Probing cell-division phenotype space and Polo-like kinase function using small molecules. Nat. Chem. Biol.2(11), 618–626 (2006).
   PubMed Web of Science ®Google Scholar
• Uckun FM. Chemosensitizing anti-cancer activity of LFM-A13, a leflunomide metabolite analog targeting Polo-like kinases. Cell Cycle6(24), 3021–3026 (2007).
   PubMed Web of Science ®Google Scholar
• Uckun FM, Dibirdik I, Qazi S et al. Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). Bioorg. Med. Chem.15(2), 800–814 (2007).
   PubMed Web of Science ®Google Scholar
• Reindl W, Yuan J, Kramer A et al. A pan-specific inhibitor of the Polo-box domains of Polo-like kinases arrests cancer cells in mitosis. Chembiochem10(7), 1145–1148 (2009).
   PubMed Web of Science ®Google Scholar
• Watanabe N, Sekine T, Takagi M et al. Deficiency in chromosome congression by the inhibition of Plk1 Polo box domain-dependent recognition. J. Biol. Chem.284(4), 2344–2353 (2009).
   PubMed Web of Science ®Google Scholar
• Santamaria A, Neef R, Eberspacher U et al. Use of the novel Plk1 inhibitor ZK-thiazolidinone to elucidate functions of Plk1 in early and late stages of mitosis. Mol. Biol. Cell.18(10), 4024–4036 (2007).
   PubMed Web of Science ®Google Scholar
• Jackson JR, Patrick DR, Dar MM et al. Targeted anti-mitotic therapies: can we improve on tubulin agents? Nat. Rev. Cancer7(2), 107–117 (2007).
   PubMed Web of Science ®Google Scholar
• Storchova Z, Breneman A, Cande J et al. genom-wide genetic analysis of polyploidy in yeast. Nature443, (7111) 541–547 (2006).
   Google Scholar
• ErskineS, Madden L, Hassler D et al. Biochemical characterization of GSK461364: A novel, potent, and selective inhibitor of Polo-like kinase-1 (Plk1) [abstract]. Proceedings of: The 98th Annual Meeting of the AACR. Philadelphia, PA, USA, 13–17 April 2007 (Abstract 3257).
   Google Scholar
• Emmitte KA, Andrews CW, Badiang JG et al. Discovery of thiophene inhibitors of Polo-like kinase. Bioorg. Med. Chem. Lett.19(3), 1018–1021 (2009).
   PubMed Web of Science ®Google Scholar
• Emmitte KA, Adjabeng GM, Andrews CW et al. Design of potent thiophene inhibitors of Polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg. Med. Chem. Lett.19(6), 1694–1697 (2009).
   PubMed Web of Science ®Google Scholar
• Von Pawel J, Reck M, Digel W et al. Randomized Phase II trial of two dosing schedules of BI 2536, a novel Plk-1 inhibitor, in patients with relapsed advanced or metastatic non-small-cell lung cancer (NSCLC) [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc.26(15 Suppl.), 8030 (2008).
   Google Scholar
• Pandha HS, Protheroe A, Wylie J et al. An open label Phase II trial of BI 2536, a novel Plk1 inhibitor, in patients with metastatic hormone refractory prostate cancer (HRPC) [abstract]. J. Clin. Oncol.ASCO Ann. Meeting Abstract Proc. Part I26(15 Suppl.), 14547 (2008).
   Google Scholar
• Bug G, Schlenk R, Müller-Tidow C et al. Phase I/II study of BI 6727 (volasertib), an intravenous Polo-like kinase-1 (Plk1) inhibitor, in patients with acute myeloid leukemia (AML): results of the dose finding for BI 6727 in combination with low-dose cytarabine Phase I/II study of BI 6727 (volasertib), in combination with low-dose cytarabine [abstract]. BloodASH Ann. Meeting Abstracts116(21), 3316 (2010).
   Google Scholar