Barasertib (AZD1152), a small molecule Aurora B inhibitor, inhibits the growth of SCLC cell lines in vitro and in vivo

Molecular Cancer Therapeutics

Volumn 15, Issue 10, 2016, Pages 2314-2322

  Helfrich, Barbara A ^a   Kim, Jihye ^a   Gao, Dexiang ^a,b   Chan, Daniel C ^a   Zhang, Zhiyong ^a   Tan, Aik Choon ^a   Bunn, Paul A ^a  

^a UNIVERSITY OF COLORADO CANCER CENTER   (United States)

^b UNIVERSITY OF COLORADO   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AURORA B KINASE; BARASERTIB; HISTONE H3; MYC PROTEIN; 2-((3-((4-((5-(2-((3-FLUOROPHENYL)AMINO)-2-OXOETHYL)-1H-PYRAZOL-3-YL)AMINO)QUINAZOLIN-7-YL)OXY)PROPYL)(ETHYL)AMINO)ETHYL DIHYDROGEN PHOSPHATE; ANTINEOPLASTIC AGENT; HISTONE; ORGANOPHOSPHATE; PROTEIN KINASE INHIBITOR; QUINAZOLINE DERIVATIVE; TRANSCRIPTOME;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFICACY; ENZYME INHIBITION; FEMALE; G2 PHASE CELL CYCLE CHECKPOINT; GENE AMPLIFICATION; GENE EXPRESSION; HISTONE PHOSPHORYLATION; HUMAN; HUMAN CELL; HUMAN TISSUE; IC50; IN VITRO STUDY; IN VIVO STUDY; LUNG CANCER CELL LINE; M PHASE CELL CYCLE CHECKPOINT; MOLECULARLY TARGETED THERAPY; MOUSE; NONHUMAN; ONCOGENE C MYC; POLYPLOIDY; PRIORITY JOURNAL; PROTEIN EXPRESSION; SHORT TANDEM REPEAT; SMALL CELL LUNG CANCER; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL PROLIFERATION; CLUSTER ANALYSIS; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; GENE EXPRESSION PROFILING; GENE EXPRESSION REGULATION; LUNG NEOPLASMS; METABOLISM; ONCOGENE MYC; PATHOLOGY; PHOSPHORYLATION; SMALL CELL LUNG CARCINOMA; TUMOR CELL LINE; TUMOR VOLUME;

ANIMALS; ANTINEOPLASTIC AGENTS; AURORA KINASE B; CELL LINE, TUMOR; CELL PROLIFERATION; CLUSTER ANALYSIS; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; GENE AMPLIFICATION; GENE EXPRESSION PROFILING; GENE EXPRESSION REGULATION, NEOPLASTIC; GENES, MYC; HISTONES; HUMANS; LUNG NEOPLASMS; MICE; ORGANOPHOSPHATES; PHOSPHORYLATION; POLYPLOIDY; PROTEIN KINASE INHIBITORS; QUINAZOLINES; SMALL CELL LUNG CARCINOMA; TRANSCRIPTOME; TUMOR BURDEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84990988111     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-16-0298     Document Type: Article

References (32)

1. Bunn PA, Minna JD, Augustyn A, Gazdar AF, Quadah Y, Krasnow MA, et al. Small cell lung cancer: can recent advances in biology and molecular biology be translated into improved outcomes? J Thoracic Oncol 2016;11:453-74.
2. Kalemkerina GP, Akerley W, Bogner P, Borghaei H, Chow L, Downey RJ, et al. Small cell lung cancer. J Natl Cmpr Cancer Netw 2011;9:1086-113.
3. El Maalouf G, Rodier J-M, Faivre S, Raymond E. Could we expect to improve survival in small cell lung cancer? Lung Cancer 2007;57 (Supp1 2):S30-S34.
4. Evans WK, Shepard FA, Feld R, Osoba D, Dang P, Doeboer G, et al. VP-16 and cisplatin as first-line therapy for small-call lung cancer. J Clin Oncol 1985;3:1471-7.
5. Rudin CM, Hann C, Peacock CD, Watkins DN. Novel systemic therapies for small cell lung cancer. J Natl Compr Can Netw 2008;6:315-22.
6. Metro G, Cappuzzo F. Emerging drugs for small-cell lung cancer. Expert Opin Emerg Drugs 2009;14:591-604.
7. Voortman J, Lee J-H, Killian JK, Suuriniemi M, Wang Y, Lucchi M, et al. Array comparative genomic hybridization-based characterization of genetic alterations in pulmonary neuroendocrine tumors. Proc Natl Acad Sci U S A 2010;107:13040-5.
8. Wistuba II, Gazdar AF, Minna JD. Molecular genetics of small cell lung carcinoma. Semin Oncol 2001;28(2 Suppl):3-13.
9. Iwakawa R, Takenaka M, Kohno T, Shimada Y, Totoki Y, Shibata T, et al. Genome-wide identification of genes with amplification and/or fusion in small cell lung cancer. Genes Chromosomes Cancer 2013;52:802-16.
10. Lok W, Klein RQ, Saif MW. Aurora kinase inhibitors as anti-cancer therapy. Anticancer Drugs 2010;21:339-50.
11. Smith SL, Boweres NL, Betticher DC, Gautschi O, Ratschiller E, Hoban PR, et al. Overexpression of aurora B kinase (AURKB) in primary non-small cell lung carcinomas is frequent, generally driven from one allele, and correlates with the level of genomic instability. Br J Cancer 2005;93:719-29.
12. Carmena M, Earnshaw WC. The cellular geography of aurora kinases. Nat Rev Mol Cell Biol 2003;4:842-54.
13. Nair JS, Ho AL, Tse AN, Coward J, Cheema H, Ambrosini G, et al. Aurora B kinase regulates the postmitotic endoreduplication checkpoint via phosphorylation of the retinoblastoma protein at serine 780. Mol Biol Cell 2009;20:2218-28.
14. Sos ML, Dietlein F, Peifer M, Schottle J, Balke-Want H, Muller C, et al. A framework for identification of actionable cancer genome dependencies in small cell lung cancer. Proc Natl Acad Sci U S A 2012;109:17034-9.
15. Melichar B, Adenis A, Lockhart AC, Bennouna J, Dees EL, Kayaleh O, et al. Safety and activity of alisertib, an investigational aurora kinase A inhibitor, in patients with breast cancer, small-cell lung cancer, non-small-cell lung cancer, head and neck squamous-cell carcinoma, and gastro-oesophageal adenocarcinoma:a five-arm phase 2 study. Lancet Oncol 2015;16:395-405.
16. Hook KE, Garza SJ, Lira ME, Ching KA, Lee NV, Cao J, et al. An integrated genomic approach to identify predictive biomarkers of response to the aurora kinase inhibitor PF-03814735. Mol Cancer Ther 2012;11:710-9.
17. Brambilla E, Gazdar A. Pathogenesis of lung cancer signaling pathways: roadmap for therapy. Eur Respir J 2009;33:1485-97.
18. de Cassia S Alves R, Meurer RT, Roehe AV. MYC amplification is associated with poor survival in small cell lung cancer: a chromogenic in situ hybridization study. J Cancer Res Clin Oncol 2014;140:2021-5
19. Frazier MW, He X, Wang J, Gu Z, Cleveland JL, Zambetti GP, et al. Activation of c-myc gene expression by tumor-derived p53 mutants requires a discrete c-terminal domain. Mol Cell Biol 1998;18:3735-43.
20. Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann J-J M, et al. Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora kinase B. J Med Chem 2007;50:2213-24.
21. Phelps RM, Johnson BE, Ihde DC, Gazdar AF, Carbonne DP, McClintock PR, et al. NCI-navy medical oncology branch cell line data base. J Cell Biochem Suppl 1996;24:32-91.
22. Chandriani S, Fregen E, Crowling VH, Pendergrass SA, Perou CM, Whitefield ML, et al. A core myc gene expression signature is prominent basal-like breast cancer but only partially overlaps with the core serum response. PLoS One 2009;4:e6693.
23. Cory AH, Owen TC, Barltrop JA, Corey JG. Use of an aqueous soluble tetrazolium/formazan assay for cell growth assays in culture. Cancer Commun 1991;3:207-12.
24. Kantargian HM, Sekeres MA, Ribrag V, Rousselot P, Garcia-Manero G, Jabbour EJ, et al. Phase I study assessing the safety and tolerability of barasertib (AZD1152) with low dose cytosine arabinoside in elderly patients with AML. Clin Lymphoma Myeloma Leuk 2013;13:559-67
25. Schwartz GK, Carvajal RD, Midgley R, Rodig SJ, Stockman PK, Ataman O, et al. Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors. Invest New Drugs 2013;31:370-80.
26. Perez-Cadahia B, Drobic B, Davie JR. H3 phosphorylation: dual role in mitosis and interphase. Biochem Cell Biol 2009;87:695-709.
27. Ditchfield C, Johnson VL, Tighe A, Ellston R, Haworth C, Johnson T, et al. Aurora B couples chromosome alignment with anaphase targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol 2003;161:267-80.
28. Gully CP, Zhang F, Chen J, Yeung JA, Velazquez-Torres G, Wang E, et al. Antineoplastic effects of an Aurora B inase inhibitor in breast cancer. Mol Cancer 2010;9:42-55.
29. Aihara A, Tanaka S, Yasen M, Matsumura S, Mitsunori Y, Murakata A, et al. The selective Aurora B kinase inhibitor AZD1152 as a novel treatment for hepatocellular carcinoma. J Heptaol 2010;52:63-71.
30. Li J, B Fang B, Kinose F, Bai Y, Kim JY, Chen YA, etal. Target identification in small cell lung cancer via integrated phenotypic screening and activity-base protein profiling. Mol Cancer Ther 2016;15:334-42.
31. Ashton S, Song YH, Nolan J, Cadogan E, Murray J, Odedra R, et al. Aurora kinase inhibitor nanoparticles target tumors with favorable therapeutic index in vivo. Sci Transl Med 2016;8:325ra17.
32. Diaz RJ, Golbourn B, Faria C, Picard D, Shih D, Raynaud D, et al. Mechanism of action and therapeutic efficacy of Aurora kinas B inhibition in MYC overexpressing medulloblastoma. Oncotarget 2015;6:3359-74.