Targeting KIT in melanoma: A paradigm of molecular medicine and targeted therapeutics

Biochemical Pharmacology

Volumn 80, Issue 5, 2010, Pages 568-574

  Woodman, Scott E ^a   Davies, Michael A ^a  

^a UNIVERSITY OF TEXAS   (United States)

Author keywords

Acral lentiginous; KIT; Melanoma; Mucosal

Indexed keywords

DASATINIB; IMATINIB; INTERLEUKIN 2; PROTEIN TYROSINE KINASE INHIBITOR; SORAFENIB; STEM CELL FACTOR RECEPTOR; TEMOZOLOMIDE;

ANAL MELANOMA; CANCER CLASSIFICATION; CANCER SURGERY; CELL MATURATION; DRUG DOSE INCREASE; DRUG DOSE REDUCTION; FEBRILE NEUTROPENIA; GENE AMPLIFICATION; GENE MUTATION; HUMAN; MELANOCYTE; MELANOMA; NONHUMAN; PRIORITY JOURNAL; REVIEW; TREATMENT RESPONSE; VAGINAL MUCOSAL MELANOMA;

ANTINEOPLASTIC AGENTS; HUMANS; MELANOMA; MUTATION; PROTO-ONCOGENE PROTEINS C-KIT; SKIN NEOPLASMS;

EID: 77954216079     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2010.04.032     Document Type: Review

References (43)

1. Besmer P., Murphy J.E., George P.C., Qiu F.H., Bergold P.J., Lederman L., et al. A new acute transforming feline retrovirus and relationship of its oncogene v-kit with the protein kinase gene family. Nature 1986, 320:415-421.
2. Yarden Y., Kuang W.J., Yang-Feng T., Coussens L., Munemitsu S., Dull T.J., et al. Human proto-oncogene c-kit: a new cell surface receptor tyrosine kinase for an unidentified ligand. EMBO J 1987, 6:3341-3351.
3. Ronnstrand L. Signal transduction via the stem cell factor receptor/c-Kit. Cell Mol Life Sci 2004, 61:2535-2548.
4. Reith A.D., Ellis C., Lyman S.D., Anderson D.M., Williams D.E., Bernstein A., et al. Signal transduction by normal isoforms and W mutant variants of the Kit receptor tyrosine kinase. EMBO J 1991, 10:2451-2459.
5. Crosier P.S., Ricciardi S.T., Hall L.R., Vitas M.R., Clark S.C., Crosier K.E. Expression of isoforms of the human receptor tyrosine kinase c-kit in leukemic cell lines and acute myeloid leukemia. Blood 1993, 82:1151-1158.
6. Huang E.J., Nocka K.H., Buck J., Besmer P. Differential expression and processing of two cell associated forms of the kit-ligand: KL-1 and KL-2. Mol Biol Cell 1992, 3:349-362.
7. Miyazawa K., Williams D.A., Gotoh A., Nishimaki J., Broxmeyer H.E., Toyama K. Membrane-bound Steel factor induces more persistent tyrosine kinase activation and longer life span of c-kit gene-encoded protein than its soluble form. Blood 1995, 85:641-649.
8. Lennartsson J., Jelacic T., Linnekin D., Shivakrupa R. Normal and oncogenic forms of the receptor tyrosine kinase kit. Stem Cells 2005, 23:16-43.
9. Corless C.L., Heinrich M.C. Molecular pathobiology of gastrointestinal stromal sarcomas. Annu Rev Pathol 2008, 3:557-586.
10. Orfao A., Garcia-Montero A.C., Sanchez L., Escribano L. Recent advances in the understanding of mastocytosis: the role of KIT mutations. Br J Haematol 2007, 138:12-30.
11. Chabot B., Stephenson D.A., Chapman V.M., Besmer P., Bernstein A. The proto-oncogene c-kit encoding a transmembrane tyrosine kinase receptor maps to the mouse W locus. Nature 1988, 335:88-89.
12. Spritz R.A., Giebel L.B., Holmes S.A. Dominant negative and loss of function mutations of the c-kit (mast/stem cell growth factor receptor) proto-oncogene in human piebaldism. Am J Hum Genet 1992, 50:261-269.
13. Geissler E.N., Ryan M.A., Housman D.E. The dominant-white spotting (W) locus of the mouse encodes the c-kit proto-oncogene. Cell 1988, 55:185-192.
14. Rossi P., Sette C., Dolci S., Geremia R. Role of c-kit in mammalian spermatogenesis. J Endocrinol Invest 2000, 23:609-615.
15. Sanders K.M., Ward S.M. Kit mutants and gastrointestinal physiology. J Physiol 2007, 578:33-42.
16. Fleischman R.A. From white spots to stem cells: the role of the Kit receptor in mammalian development. Trends Genet 1993, 9:285-290.
17. Huang S., Luca M., Gutman M., McConkey D.J., Langley K.E., Lyman S.D., et al. Enforced c-KIT expression renders highly metastatic human melanoma cells susceptible to stem cell factor-induced apoptosis and inhibits their tumorigenic and metastatic potential. Oncogene 1996, 13:2339-2347.
18. Lassam N., Bickford S. Loss of c-kit expression in cultured melanoma cells. Oncogene 1992, 7:51-56.
19. Went P.T., Dirnhofer S., Bundi M., Mirlacher M., Schraml P., Mangialaio S., et al. Prevalence of KIT expression in human tumors. J Clin Oncol 2004, 22:4514-4522.
20. Willmore-Payne C., Holden J.A., Tripp S., Layfield L.J. Human malignant melanoma: detection of BRAF- and c-kit-activating mutations by high-resolution amplicon melting analysis. Hum Pathol 2005, 36:486-493.
21. Willmore-Payne C., Holden J.A., Hirschowitz S., Layfield L.J. BRAF and c-kit gene copy number in mutation-positive malignant melanoma. Hum Pathol 2006, 37:520-527.
22. Curtin J.A., Fridlyand J., Kageshita T., Patel H.N., Busam K.J., Kutzner H., et al. Distinct sets of genetic alterations in melanoma. N Engl J Med 2005, 353:2135-2147.
23. Curtin J.A., Busam K., Pinkel D., Bastian B.C. Somatic activation of KIT in distinct subtypes of melanoma. J Clin Oncol 2006, 24:4340-4346.
24. Antonescu C.R., Busam K.J., Francone T.D., Wong G.C., Guo T., Agaram N.P., et al. L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition. Int J Cancer 2007, 121:257-264.
25. Ashida A., Takata M., Murata H., Kido K., Saida T. Pathological activation of KIT in metastatic tumors of acral and mucosal melanomas. Int J Cancer 2009, 124:862-868.
26. Beadling C., Jacobson-Dunlop E., Hodi F.S., Le C., Warrick A., Patterson J., et al. KIT gene mutations and copy number in melanoma subtypes. Clin Cancer Res 2008, 14:6821-6828.
27. Rivera R.S., Nagatsuka H., Gunduz M., Cengiz B., Gunduz E., Siar C.H., et al. C-kit protein expression correlated with activating mutations in KIT gene in oral mucosal melanoma. Virchows Arch 2008, 452:27-32.
28. Satzger I., Schaefer T., Kuettler U., Broecker V., Voelker B., Ostertag H., et al. Analysis of c-KIT expression and KIT gene mutation in human mucosal melanomas. Br J Cancer 2008, 99:2065-2069.
29. Torres-Cabala C.A., Wang W.L., Trent J., Yang D., Chen S., Galbincea J., et al. Correlation between KIT expression and KIT mutation in melanoma: a study of 173 cases with emphasis on the acral-lentiginous/mucosal type. Mod Pathol 2009, 22:1446-1456.
30. Jiang X., Zhou J., Yuen N.K., Corless C.L., Heinrich M.C., Fletcher J.A., et al. Imatinib targeting of KIT-mutant oncoprotein in melanoma. Clin Cancer Res 2008, 14:7726-7732.
31. Alexeev V., Yoon K. Distinctive role of the cKit receptor tyrosine kinase signaling in mammalian melanocytes. J Invest Dermatol 2006, 126:1102-1110.
32. Monsel G., Ortonne N., Bagot M., Bensussan A., Dumaz N. c-Kit mutants require hypoxia-inducible factor 1alpha to transform melanocytes. Oncogene 2010, 29:227-236.
33. Bougherara H., Subra F., Crepin R., Tauc P., Auclair C., Poul M.A. The aberrant localization of oncogenic kit tyrosine kinase receptor mutants is reversed on specific inhibitory treatment. Mol Cancer Res 2009, 7:1525-1533.
34. Tsao H., Atkins M.B., Sober A.J. Management of cutaneous melanoma. N Engl J Med 2004, 351:998-1012.
35. Kim K.B., Eton O., Davis D.W., Frazier M.L., McConkey D.J., Diwan A.H., et al. Phase II trial of imatinib mesylate in patients with metastatic melanoma. Br J Cancer 2008, 99:734-740.
36. Ugurel S., Hildenbrand R., Zimpfer A., La Rosee P., Paschka P., Sucker A., et al. Lack of clinical efficacy of imatinib in metastatic melanoma. Br J Cancer 2005, 92:1398-1405.
37. Wyman K., Atkins M.B., Prieto V., Eton O., McDermott D.F., Hubbard F., et al. Multicenter Phase II trial of high-dose imatinib mesylate in metastatic melanoma: significant toxicity with no clinical efficacy. Cancer 2006, 106:2005-2011.
38. Lutzky J., Bauer J., Bastian B.C. Dose-dependent, complete response to imatinib of a metastatic mucosal melanoma with a K642E KIT mutation. Pigment Cell Melanoma Res 2008, 21:492-493.
39. Quintas-Cardama A., Lazar A.J., Woodman S.E., Kim K., Ross M., Hwu P. Complete response of stage IV anal mucosal melanoma expressing KIT Val560Asp to the multikinase inhibitor sorafenib. Nat Clin Pract Oncol 2008, 5:737-740.
40. Hodi F.S., Friedlander P., Corless C.L., Heinrich M.C., Mac Rae S., Kruse A., et al. Major response to imatinib mesylate in KIT-mutated melanoma. J Clin Oncol 2008, 26:2046-2051.
41. Woodman S.E., Trent J.C., Stemke-Hale K., Lazar A.J., Pricl S., Pavan G.M., et al. Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates. Mol Cancer Ther 2009, 8:2079-2085.
42. Carvajal R.D., Chapman P.B., Wolchok J.D., Cane L., Teitcher J.B., Lutzky J., et al. A phase II study of imatinib mesylate (IM) for patients with advanced melanoma harboring somatic alterations of KIT. J Clin Oncol 2009, 27. (suppl; abstr 9001).
43. Fisher D.E., Barnhill R., Hodi F.S., Herlyn M., Merlino G., Medrano E., et al. Melanoma from bench to bedside: meeting report from the 6th international melanoma congress. Pigment Cell Melanoma Res 2010, 23:14-26.