Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer

Oncotarget

Volumn 3, Issue 12, 2012, Pages 1629-1640

  Chung, Suyoun ^a   Suzuki, Hanae ^b   Miyamoto, Takashi ^b   Takamatsu, Naofumi ^b   Tatsuguchi, Ayako ^c   Ueda, Koji ^c   Kijima, Kyoko ^b   Nakamura, Yusuke ^a,d   Matsuo, Yo ^b  

^a UNIVERSITY OF CHICAGO   (United States)

^b Research and Development Division   (Japan)

^c RIKEN   (Japan)

^d UNIVERSITY OF TOKYO   (Japan)

Author keywords

Cancer stem cell; Drug discovery; Kinase inhibitor; Oncogene

Indexed keywords

1 [6 (3,5 DICHLORO 4 HYDROXYPHENYL) 4 [[TRANS 4 [(DIMETHYLAMINO)METHYL]CYCLOHEXYL]AMINO] 1,5 NAPHTHYRIDIN 3 YL]ETHANONE; DREBRIN; DREBRIN LIKE PROTEIN; MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE; MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE INHIBITOR; OTSSP 167; PROTEASOME; PROTEASOME SUBUNIT ALPHA TYPE 1; PROTEIN SERINE THREONINE KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CANCER CELL; CANCER INHIBITION; CELL INVASION; CONTROLLED STUDY; DRUG DOSE COMPARISON; DRUG STRUCTURE; ENZYME INHIBITION; FEMALE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; LUNG CANCER; LUNG TUMOR; MALE; MOUSE; NONHUMAN; PANCREAS CANCER; PROSTATE CANCER; PROTEIN PHOSPHORYLATION; STRUCTURE ACTIVITY RELATION; TRIPLE NEGATIVE BREAST CANCER; TUMOR XENOGRAFT;

EID: 84874680562     PISSN: None     EISSN: 19492553     Source Type: Journal    
DOI: 10.18632/oncotarget.790     Document Type: Article

References (41)

1. Jemal A, Siegel R, Ward E, Hao Y, Xu J, Murray T, Thun MJ. Cancer statistics, 2008. CA Cancer J Clin. 2008; 58:71-96.
2. Forouzanfar MH, Foreman KJ, Delossantos AM, Lozano R, Lopez AD, Murray CJ, Naghavi M. Breast and cervical cancer in 187 countries between 1980 and 2010: A systematic analysis. Lancet. 2011; 378:1461-1484.
3. Sotiriou C, Pusztai L. Gene-expression signatures in breast cancer. N Engl J Med. 2009; 360:790-800.
4. Rakha EA, Elsheikh SE, Aleskandarany MA, Habashi HO, Green AR, Powe DG, El-Sayed ME, Benhasouna A, Brunet JS, Akslen LA, Evans AJ, Blamey R, Reis-Filho JS, Foulkes WD, Ellis IO. Triple-negative breast cancer: Distinguishing between basal and nonbasal subtypes. Clin Cancer Res. 2009; 15:2302-2310.
5. Griffiths CL, Olin JL. Triple negative breast cancer: A brief review of its characteristics and treatment options. J Pharm Pract. 25:319-323.
6. Cleator S, Heller W, Coombes RC. Triple-negative breast cancer: Therapeutic options. Lancet Oncol. 2007; 8:235-244.
7. Foulkes WD, Smith IE, Reis-Filho JS. Triple-negative breast cancer. N Engl J Med. 2010; 363:1938-1948.
8. Heyer BS, Warsowe J, Solter D, Knowles BB, Ackerman SL. New member of the snf1/ampk kinase family, melk, is expressed in the mouse egg and preimplantation embryo. Mol Reprod Dev. 1997; 47:148-156.
9. Lin ML, Park JH, Nishidate T, Nakamura Y, Katagiri T. Involvement of maternal embryonic leucine zipper kinase (melk) in mammary carcinogenesis through interaction with bcl-g, a pro-apoptotic member of the bcl-2 family. Breast Cancer Res. 2007; 9:R17.
10. Gray D, Jubb AM, Hogue D, Dowd P, Kljavin N, Yi S, Bai W, Frantz G, Zhang Z, Koeppen H, de Sauvage FJ, Davis DP. Maternal embryonic leucine zipper kinase/murine protein serine-threonine kinase 38 is a promising therapeutic target for multiple cancers. Cancer Res. 2005; 65:9751-9761.
11. Bianchini G, Iwamoto T, Qi Y, Coutant C, Shiang CY, Wang B, Santarpia L, Valero V, Hortobagyi GN, Symmans WF, Gianni L, Pusztai L. Prognostic and therapeutic implications of distinct kinase expression patterns in different subtypes of breast cancer. Cancer Res. 2010; 70:8852-8862.
12. Sutter R, Yadirgi G, Marino S. Neural stem cells, tumour stem cells and brain tumours: Dangerous relationships? Biochim Biophys Acta. 2007; 1776:125-137.
13. Hebbard LW, Maurer J, Miller A, Lesperance J, Hassell J, Oshima RG, Terskikh AV. Maternal embryonic leucine zipper kinase is upregulated and required in mammary tumor-initiating cells in vivo. Cancer Res. 2010; 70:8863-8873.
14. Rich JN. Cancer stem cells in radiation resistance. Cancer Res. 2007; 67:8980-8984.
15. Dean M, Fojo T, Bates S. Tumour stem cells and drug resistance. Nat Rev Cancer. 2005; 5:275-284.
16. Kemper K, Grandela C, Medema JP. Molecular identification and targeting of colorectal cancer stem cells. Oncotarget. 2010; 1:387-395.
17. Curtin JC, Lorenzi MV. Drug discovery approaches to target wnt signaling in cancer stem cells. Oncotarget. 2010; 1:563-577.
18. Nakano I, Masterman-Smith M, Saigusa K, Paucar AA, Horvath S, Shoemaker L, Watanabe M, Negro A, Bajpai R, Howes A, Lelievre V, Waschek JA, Lazareff JA, Freije WA, Liau LM, Gilbertson RJ, et al. Maternal embryonic leucine zipper kinase is a key regulator of the proliferation of malignant brain tumors, including brain tumor stem cells. J Neurosci Res. 2008; 86:48-60.
19. Sportsman JR, Gaudet EA, Boge A. Immobilized metal ion affinity-based fluorescence polarization (imap): Advances in kinase screening. Assay Drug Dev Technol. 2004; 2:205-214.
20. Larbolette O, Wollscheid B, Schweikert J, Nielsen PJ, Wienands J. Sh3p7 is a cytoskeleton adapter protein and is coupled to signal transduction from lymphocyte antigen receptors. Mol Cell Biol. 1999; 19:1539-1546.
21. Mise-Omata S, Montagne B, Deckert M, Wienands J, Acuto O. Mammalian actin binding protein 1 is essential for endocytosis but not lamellipodia formation: Functional analysis by rna interference. Biochem Biophys Res Commun. 2003; 301:704-710.
22. Kessels MM, Engqvist-Goldstein AE, Drubin DG, Qualmann B. Mammalian abp1, a signal-responsive f-actin-binding protein, links the actin cytoskeleton to endocytosis via the gtpase dynamin. J Cell Biol. 2001; 153:351-366.
23. Cohen P, Holmes CF, Tsukitani Y. Okadaic acid: A new probe for the study of cellular regulation. Trends Biochem Sci. 1990; 15:98-102.
24. Yamaguchi K, Hata K, Wada T, Moriya S, Miyagi T. Epidermal growth factor-induced mobilization of a ganglioside-specific sialidase (neu3) to membrane ruffles. Biochem Biophys Res Commun. 2006; 346:484-490.
25. Deng S, Zhou H, Xiong R, Lu Y, Yan D, Xing T, Dong L, Tang E, Yang H. Over-expression of genes and proteins of ubiquitin specific peptidases (usps) and proteasome subunits (pss) in breast cancer tissue observed by the methods of rfdd-pcr and proteomics. Breast Cancer Res Treat. 2007; 104:21-30.
26. He X, Gonzalez V, Tsang A, Thompson J, Tsang TC, Harris DT. Differential gene expression profiling of cd34+ cd133+ umbilical cord blood hematopoietic stem progenitor cells. Stem Cells Dev. 2005; 14:188-198.
27. Zhang Z, Stiegler AL, Boggon TJ, Kobayashi S, Halmos B. Egfr-mutated lung cancer: A paradigm of molecular oncology. Oncotarget. 2010; 1:497-514.
28. Zhang J, Yang PL, Gray NS. Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer. 2009; 9:28-39.
29. Schmidt-Kittler O, Zhu J, Yang J, Liu G, Hendricks W, Lengauer C, Gabelli SB, Kinzler KW, Vogelstein B, Huso DL, Zhou S. Pi3kalpha inhibitors that inhibit metastasis. Oncotarget. 2010; 1:339-348.
30. Liu-Sullivan N, Zhang J, Bakleh A, Marchica J, Li J, Siolas D, Laquerre S, Degenhardt YY, Wooster R, Chang K, Hannon GF, Powers S. Pooled shrna screen for sensitizers to inhibition of the mitotic regulator polo-like kinase (plk1). Oncotarget. 2011; 2:1254-1264.
31. Hantschel O, Grebien F, Superti-Furga G. Targeting allosteric regulatory modules in oncoproteins: «Drugging the undruggable». Oncotarget. 2011; 2:828-829.
32. Crespo A, Zhang X, Fernandez A. Redesigning kinase inhibitors to enhance specificity. J Med Chem. 2008; 51:4890-4898.
33. Morachis JM, Huang R, Emerson BM. Identification of kinase inhibitors that target transcription initiation by rna polymerase ii. Oncotarget. 2011; 2:18-28.
34. Le Bras S, Foucault I, Foussat A, Brignone C, Acuto O, Deckert M. Recruitment of the actin-binding protein hip-55 to the immunological synapse regulates t cell receptor signaling and endocytosis. J Biol Chem. 2004; 279:15550-15560.
35. Friedl P, Locker J, Sahai E, Segall JE. Classifying collective cancer cell invasion. Nat Cell Biol. 2012; 14:777-783.
36. Li X, Wolf ME. Visualization of virus-infected brain regions using a gfp-illuminating flashlight enables accurate and rapid dissection for biochemical analysis. J Neurosci Methods. 2011; 201:177-179.
37. Hermeking H. The 14-3-3 cancer connection. Nat Rev Cancer. 2003; 3:931-943.
38. Murata S, Yashiroda H, Tanaka K. Molecular mechanisms of proteasome assembly. Nat Rev Mol Cell Biol. 2009; 10:104-115.
39. Bose S, Stratford FL, Broadfoot KI, Mason GG, Rivett AJ. Phosphorylation of 20s proteasome alpha subunit c8 (alpha7) stabilizes the 26s proteasome and plays a role in the regulation of proteasome complexes by gamma-interferon. Biochem J. 2004; 378:177-184.
40. Vilchez D, Boyer L, Morantte I, Lutz M, Merkwirth C, Joyce D, Spencer B, Page L, Masliah E, Berggren WT, Gage FH, Dillin A. Increased proteasome activity in human embryonic stem cells is regulated by psmd11. Nature. 2012; 489:304-308.
41. Fukukawa C, Hanaoka H, Nagayama S, Tsunoda T, Toguchida J, Endo K, Nakamura Y, Katagiri T. Radioimmunotherapy of human synovial sarcoma using a monoclonal antibody against fzd10. Cancer Sci. 2008; 99:432-440.