Activating the Wnt/β-catenin pathway for the treatment of melanoma - Application of LY2090314, a Novel selective inhibitor of glycogen synthase kinase-3

PLoS ONE

Volumn 10, Issue 4, 2015, Pages

  Atkinson, Jennifer M ^a   Rank, Kenneth B ^a   Zeng, Yi ^a   Capen, Andrew ^a   Yadav, Vipin ^a   Manro, Jason R ^a   Engler, Thomas A ^a   Chedid, Marcio ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AXIN; AXIN2 PROTEIN; B RAF KINASE; BETA CATENIN; CASPASE 3; CASPASE 7; DACARBAZINE; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; LY 2090314; MESSENGER RNA; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; RAS PROTEIN; SHORT HAIRPIN RNA; UNCLASSIFIED DRUG; VEMURAFENIB; WNT PROTEIN; 3-(9-FLUORO-2-(PIPERIDIN-1-YLCARBONYL)-1,2,3,4-TETRAHYDRO(1,4)DIAZEPINO(6,7,1-HI)INDOL-7-YL)-4-IMIDAZO(1,2-A)PYRIDIN-3-YL-1H-PYRROLE-2,5-DIONE; ANTINEOPLASTIC AGENT; FUSED HETEROCYCLIC RINGS; GLYCOGEN SYNTHASE KINASE 3; MALEIMIDE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; AXIN2 GENE; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG POTENCY; DRUG POTENTIATION; ENZYME ACTIVATION; ENZYME INHIBITION; FEMALE; GENE EXPRESSION REGULATION; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; INTRACELLULAR SIGNALING; MELANOMA; MELANOMA CELL LINE; MOUSE; NONHUMAN; PROTEIN CLEAVAGE; PROTEIN EXPRESSION; TUMOR XENOGRAFT; WNT SIGNALING PATHWAY; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL PROLIFERATION; DRUG EFFECTS; DRUG RESISTANCE; DRUG SCREENING; GENETICS; METABOLISM; NUDE MOUSE; SKIN NEOPLASMS; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL LINE, TUMOR; CELL PROLIFERATION; DRUG RESISTANCE, NEOPLASM; FEMALE; GLYCOGEN SYNTHASE KINASE 3; HETEROCYCLIC COMPOUNDS, 3-RING; HUMANS; MALEIMIDES; MELANOMA; MICE; MICE, NUDE; SKIN NEOPLASMS; WNT SIGNALING PATHWAY; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84928567857     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0125028     Document Type: Article

References (32)

1. Jemal A, Bray F, Center MM, Ferlay J, Ward E, Forman D (2011) Global cancer statistics. CA Cancer J Clin 61: 69-90. doi: 10.3322/caac.20107 PMID: 21296855
2. FDA (2011) FDA approves Zelboraf and companion diagnostic test for late-stage skin cancer In: Jefferson E, editor. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm268241.htm: FDA.
3. Hodis E, Watson IR, Kryukov GV, Arold ST, Imielinski M, Theurillat JP, et al. (2012) A landscape of driver mutations in melanoma. Cell 150: 251-263. doi: 10.1016/j.cell.2012.06.024 PMID: 22817889
4. Wagle N, Emery C, Berger MF, Davis MJ, Sawyer A, Pochanard P, et al. (2011) Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol 29: 3085-3096. doi: 10.1200/JCO.2010.33.2312 PMID: 21383288
5. Flaherty KT, Infante JR, Daud A, Gonzalez R, Kefford RF, Sosman J, et al. (2012) Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med 367: 1694-1703. doi: 10.1056/NEJMoa1210093 PMID: 23020132
6. Liu C, Li Y, Semenov M, Han C, Baeg GH, Tan Y, et al. (2002) Control of beta-catenin phosphorylation/degradation by a dual-kinase mechanism. Cell 108: 837-847. PMID: 11955436
7. Aberle H, Bauer A, Stappert J, Kispert A, Kemler R (1997) beta-catenin is a target for the ubiquitin-proteasome pathway. EMBO J 16: 3797-3804. PMID: 9233789
8. Kitagawa M, Hatakeyama S, Shirane M, Matsumoto M, Ishida N, Hattori K, et al. (1999) An F-box protein, FWD1, mediates ubiquitin-dependent proteolysis of beta-catenin. EMBO J 18: 2401-2410. PMID: 10228155
9. Li VS, Ng SS, Boersema PJ, Low TY, Karthaus WR, Gerlach JP, et al. (2012) Wnt signaling through inhibition of beta-catenin degradation in an intact Axin1 complex. Cell 149: 1245-1256. doi: 10.1016/j.cell.2012.05.002 PMID: 22682247
10. Clevers H, Nusse R (2012) Wnt/beta-catenin signaling and disease. Cell 149: 1192-1205. doi: 10.1016/j.cell.2012.05.012 PMID: 22682243
11. Scholer-Dahirel A, Schlabach MR, Loo A, Bagdasarian L, Meyer R, Guo R, et al. (2011) Maintenance of adenomatous polyposis coli (APC)-mutant colorectal cancer is dependent on Wnt/beta-catenin signaling. Proc Natl Acad Sci U S A 108: 17135-17140. doi: 10.1073/pnas.1104182108 PMID: 21949247
12. Liu CC, Prior J, Piwnica-Worms D, Bu G (2010) LRP6 overexpression defines a class of breast cancer subtype and is a target for therapy. Proc Natl Acad Sci U S A 107: 5136-5141. doi: 10.1073/pnas.0911220107 PMID: 20194742
13. Anastas JN, Moon RT (2013) WNT signalling pathways as therapeutic targets in cancer. Nat Rev Cancer 13: 11-26. doi: 10.1038/nrc3419 PMID: 23258168
14. Fattet S, Haberler C, Legoix P, Varlet P, Lellouch-Tubiana A, Lair S, et al. (2009) Beta-catenin status in paediatric medulloblastomas: correlation of immunohistochemical expression with mutational status, genetic profiles, and clinical characteristics. J Pathol 218: 86-94. doi: 10.1002/path.2514 PMID: 19197950
15. Horvath LG, Henshall SM, Lee CS, Kench JG, Golovsky D, Brenner PC, et al. (2005) Lower levels of nuclear beta-catenin predict for a poorer prognosis in localized prostate cancer. Int J Cancer 113: 415-422. PMID: 15455387
16. Chien AJ, Moore EC, Lonsdorf AS, Kulikauskas RM, Rothberg BG, Berger AJ, et al. (2009) Activated Wnt/beta-catenin signaling in melanoma is associated with decreased proliferation in patient tumors and a murine melanoma model. Proc Natl Acad Sci U S A 106: 1193-1198. doi: 10.1073/pnas.0811902106 PMID: 19144919
17. Kageshita T, Hamby CV, Ishihara T, Matsumoto K, Saida T, Ono T (2001) Loss of beta-catenin expression associated with disease progression in malignant melanoma. Br J Dermatol 145: 210-216. PMID: 11531781
18. Lucero OM, Dawson DW, Moon RT, Chien AJ (2010) A re-evaluation of the "oncogenic" nature of Wnt/ beta-catenin signaling in melanoma and other cancers. Curr Oncol Rep 12: 314-318. doi: 10.1007/s11912-010-0114-3 PMID: 20603725
19. Arozarena I, Bischof H, Gilby D, Belloni B, Dummer R, Wellbrock C (2011) In melanoma, beta-catenin is a suppressor of invasion. Oncogene 30: 4531-4543. doi: 10.1038/onc.2011.162 PMID: 21577209
20. Sinnberg T, Menzel M, Ewerth D, Sauer B, Schwarz M, Schaller M, et al. (2011) beta-Catenin signaling increases during melanoma progression and promotes tumor cell survival and chemoresistance. PLoS One 6: e23429. doi: 10.1371/journal.pone.0023429 PMID: 21858114
21. Gallagher SJ, Rambow F, Kumasaka M, Champeval D, Bellacosa A, Delmas V, et al. (2012) Beta-catenin inhibits melanocyte migration but induces melanoma metastasis. Oncogene.
22. Biechele TL, Camp ND, Fass DM, Kulikauskas RM, Robin NC, White BD, et al. (2010) Chemical-genetic screen identifies riluzole as an enhancer of Wnt/beta-catenin signaling in melanoma. Chem Biol 17: 1177-1182. doi: 10.1016/j.chembiol.2010.08.012 PMID: 21095567
23. Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, et al. (2004) Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. J Med Chem 47: 3934-3937. PMID: 15267232
24. Bafico A, Gazit A, Wu-Morgan SS, Yaniv A, Aaronson SA (1998) Characterization of Wnt-1 and Wnt-2 induced growth alterations and signaling pathways in NIH3T3 fibroblasts. Oncogene 16: 2819-2825. PMID: 9652750
25. Williams SP, Nowicki MO, Liu F, Press R, Godlewski J, Abdel-Rasoul M, et al. (2011) Indirubins decrease glioma invasion by blocking migratory phenotypes in both the tumor and stromal endothelial cell compartments. Cancer Res 71: 5374-5380. doi: 10.1158/0008-5472.CAN-10-3026 PMID: 21697283
26. He TC, Sparks AB, Rago C, Hermeking H, Zawel L, da Costa LT, et al. (1998) Identification of c-MYC as a target of the APC pathway. Science 281: 1509-1512. PMID: 9727977
27. Wang Z, Iwasaki M, Ficara F, Lin C, Matheny C, Wong SH, et al. (2010) GSK-3 promotes conditional association of CREB and its coactivators with MEIS1 to facilitate HOX-mediated transcription and oncogenesis. Cancer Cell 17: 597-608. doi: 10.1016/j.ccr.2010.04.024 PMID: 20541704
28. Doble BW, Patel S, Wood GA, Kockeritz LK, Woodgett JR (2007) Functional redundancy of GSK-3alpha and GSK-3beta in Wnt/beta-catenin signaling shown by using an allelic series of embryonic stem cell lines. Dev Cell 12: 957-971. PMID: 17543867
29. Yadav V, Zhang X, Liu J, Estrem S, Li S, Gong XQ, et al. (2012) Reactivation of Mitogen-Activated Protein Kinase (MAPK) Pathway by FGF Receptor 3 (FGFR3)/Ras Mediates Resistance to Vemurafenib in Human B-RAF V600E Mutant Melanoma. J Biol Chem.
30. Yamanaka H, Moriguchi T, Masuyama N, Kusakabe M, Hanafusa H, Takada R, et al. (2002) JNK functions in the non-canonical Wnt pathway to regulate convergent extension movements in vertebrates. EMBO Rep 3: 69-75. PMID: 11751577
31. Nateri AS, Spencer-Dene B, Behrens A (2005) Interaction of phosphorylated c-Jun with TCF4 regulates intestinal cancer development. Nature 437: 281-285. PMID: 16007074
32. Biechele TL, Kulikauskas RM, Toroni RA, Lucero OM, Swift RD, James RG, et al. (2012) Wnt/beta-catenin signaling and AXIN1 regulate apoptosis triggered by inhibition of the mutant kinase BRAFV600E in human melanoma. Sci Signal 5: ra3.