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Expert Opinion on Drug Discovery Volume 4, 2009 - Issue 4
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Reviews

The future of targeted therapy approaches in melanoma

Liliana P Cantini The Molecular Oncology Program and Comprehensive Melanoma Research Center, The Moffitt Cancer Center, 12902 Magnolia Drive, Tampa, FL, 33612, USA
, PhD,
Friedegund Meier University of Tuebingen, Division of Dermatologic Oncology, Department of Dermatology, Tuebingen, Germany
, MD,
Vernon K Sondak University of South Florida College of Medicine, The Moffitt Cancer Center, Department of Oncologic Sciences, Department of Cutaneous Oncology, Tampa, FL, USA +1 813 746 8725; +1 813 747 4384; [email protected]
, MD &
Keiran SM Smalley The Molecular Oncology Program and Comprehensive Melanoma Research Center, The Moffitt Cancer Center, 12902 Magnolia Drive, Tampa, FL, 33612, USA; University of South Florida College of Medicine, The Moffitt Cancer Center, Department of Oncologic Sciences, Department of Cutaneous Oncology, Tampa, FL, USA +1 813 746 8725; +1 813 747 4384; [email protected]
, PhD
Pages 445-456 | Published online: 03 Apr 2009

Bibliography

  • Slominski A, Wortsman J, Carlson AJ, et al. Malignant melanoma - an update. Arch Pathol Lab Med 2001;125(10):1295-306
  • Balch CM, Buzaid AC, Atkins MB, et al. A new American joint committee on cancer staging system for cutaneous melanoma. Cancer 2000;88(6):1484-91
  • Atkins MB, Sosman JA. The role of cytotoxic chemotherapeutic agents either alone or in combination with biological response modifiers, p1-2. Waltham MA: UpToDate, 2007
  • Soengas MS, Lowe SW. Apoptosis and melanoma chemoresistance. Oncogene 2003;22(20):3138-51
  • Druker BJ, Talpaz M, Resta DJ, et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 2001;344(14):1031-7
  • Pao W, Miller V, Zakowski M, et al. EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci USA 2004;101(36):13306-11
  • Brose MS, Volpe P, Kumar M, et al. BRAF and RAS mutations inhuman lung cancer and melanoma. Am J Hum Genet 2002;71(4):246
  • Kitamura Y, Hirotab S. Kit as a human oncogenic tyrosine kinase. Cell Mol Life Sci 2004;61(23):2924-31
  • Davies H, Bignell GR, Cox C, et al. Mutations of the BRAF gene in human cancer. Nature 2002;417(6892):949-54
  • Wan PT, Garnett MJ, Roe SM, et al. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell 2004;116(6):855-67
  • Sherr CJ. Cell cycle control and cancer. Harvey Lect 2000;96:73-92
  • Smalley KSM. A pivotal role for ERK in the oncogenic behaviour of malignant melanoma? Int J Cancer 2003;104(5):527-32
  • Sherr CJ. G1 phase progression: cycling on cue. Cell 1994;79(4):551-5
  • Bhatt KV, Spofford LS, Aram G, et al. Adhesion control of cyclin D1 and p27Kip1 levels is deregulated in melanoma cells through BRAF-MEK-ERK signaling. Oncogene 2005;24(21):3459-71
  • Haass NK, Sproesser K, Nguyen TK, et al. The mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor AZD6244 (ARRY-142886) induces growth arrest in melanoma cells and tumor regression when combined with docetaxel. Clin Cancer Res 2008;14(1):230-9
  • McDaid HM, Lopez-Barcons L, Grossman A, et al. Enhancement of the therapeutic efficacy of taxol by the mitogen-activated protein kinase kinase inhibitor CI-1040 in nude mice bearing human heterotransplants. Cancer Res 2005;65(7):2854-60
  • Hingorani SR, Jacobetz MA, Robertson GP, et al. Suppression of BRAF(V599E) in human melanoma abrogates transformation. Cancer Res 2003;63(17):5198-202
  • King AJ, Patrick DR, Batorsky RS, et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res 2006;66(23):11100-5
  • Tsai J, Lee JT, Wang W, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci USA 2008;105(8):3041-6
  • Solit DB, Garraway LA, Pratilas CA, et al. BRAF mutation predicts sensitivity to MEK inhibition. Nature 2006;439(7074):358-62
  • Wilhelm SM, Carter C, Tang L, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 2004;64(19):7099-109
  • Sharma A, Trivedi NR, Zimmerman MA, et al. Mutant V599EB-Raf regulates growth and vascular development of malignant melanoma tumors. Cancer Res 2005;65(6):2412-21
  • Eisen T, Ahmad T, Flaherty KT, et al. Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis. Br J Cancer 2006;95(5):581-6
  • Flaherty KT, Schiller J, Schuchter LM, et al. A phase I trial of the oral, multikinase inhibitor sorafenib in combination with carboplatin and paclitaxel. Clin Cancer Res 2008;14(15):4836-42
  • Smalley KS, Lioni M, Palma MD, et al. Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas. Mol Cancer Ther 2008;7(9):2876-83
  • Ellerhorst JA, Ekmekcioglu S, Johnson MK, et al. Regulation of iNOS by the p44/42 mitogen-activated protein kinase pathway in human melanoma. Oncogene 2006;25(28):3956-62
  • Zhang XD, Borrow JM, Zhang XY, et al. Activation of ERK1/2 protects melanoma cells from TRAIL-induced apoptosis by inhibiting Smac/DIABLO release from mitochondria. Oncogene 2003;22(19):2869-81
  • Woods D, Cherwinski H, Venetsanakos E, et al. Induction of beta 3-integrin gene expression by sustained activation of the Ras-regulated Raf-MEK-extracellular signal-regulated kinase signaling pathway. Mol Cell Biol 2001;21(9):3192-205
  • Karasarides M, Chiloeches A, Hayward R, et al. B-RAF is a therapeutic target in melanoma. Oncogene 2004;23(37):6292-8
  • Tsao H, Zhang X, Fowlkes K, Haluska FG. Relative reciprocity of NRAS and PTEN/MMAC1 alterations in cutaneous melanoma cell lines. Cancer Res 2000;60(7):1800-4
  • Curtin JA, Busam K, Pinkel D, Bastian BC. Somatic activation of KIT in distinct subtypes of melanoma. J Clin Oncol 2006;24(26):4340-6
  • Lin WM, Baker AC, Beroukhim R, et al. Modeling genomic diversity and tumor dependency in malignant melanoma. Cancer Res 2008;68(3):664-73
  • Smalley KS, Contractor R, Nguyen TK, et al. Identification of a novel subgroup of melanomas with KIT/cyclin-dependent kinase-4 overexpression. Cancer Res 2008;68(14):5743-52
  • Adjei AA, Cohen RB, Franklin W, et al. Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers. J Clin Oncol 2008;26(13):2139-46
  • Dummer R, Robert C, Chapman PB, et al. AZD6244 (ARRY-142886) vs temozolomide (TMZ) in patients with advanced melanoma: an open-label, randomized, multicenter, phase II study [abstract 9033]. J Clin Oncol 2008;26
  • Houben R, Vetter-Kauczok CS, Ortmann S, et al. Phospho-ERK staining is a poor indicator of the mutational status of BRAF and NRAS in human melanoma. J Invest Dermatol 2008;128(8):2013-23
  • Houben R, Ortmann S, Drasche A, et al. Proliferation arrest in B-Raf mutant melanoma cell lines upon MAPK pathway activation. J Invest Dermatol 2009;129(2):406-14
  • Wang Y, Van Becelaere K, Jiang P, et al. A role for K-ras in conferring resistance to the MEK inhibitor, CI-1040. Neoplasia 2005;7(4):336-47
  • Montagut C, Sharma SV, Shioda T, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res 2009;129(2):406-14
  • Satyamoorthy K, Li G, Vaidya B, et al. Insulin-like growth factor-1 induces survival and growth of biologically early melanoma cells through both the mitogen-activated protein kinase and beta-catenin pathways. Cancer Res 2001;61(19):7318-24
  • Curtin JA, Stark MS, Pinkel D, et al. PI3-Kinase subunits are infrequent somatic targets in melanoma. J Invest Dermatol 2006;126(7):1660-3
  • Waldmann V, Wacker J, Deichmann M. Absence of mutations in the pleckstrin homology (PH) domain of protein kinase B (PKB/Akt) in malignant melanoma. Melanoma Res 2002;12(1):45-50
  • Waldmann V, Wacker J, Deichmann M. Mutations of the activation-associated phosphorylation sites at codons 308 and 473 of protein kinase B are absent in human melanoma. Arch Dermatol Res 2001;293(7):368-72
  • Li J, Yen C, Liaw D, et al. PTEN, a putative protein tyrosine phosphatase gene mutated in human brain, breast, and prostate cancer. Science 1997;275(5308):1943-7
  • Steck PA, Pershouse MA, Jasser SA, et al. Identification of a candidate tumour suppressor gene, MMAC1, at chromosome 10q23.3 that is mutated in multiple advanced cancers. Nat Genet 1997;15(4):356-62
  • Tsao H, Atkins MB, Sober AJ. Management of cutaneous melanoma. N Engl J Med 2004;351(10):998-1012
  • Guldberg P, thor Straten P, Birck A, et al. Disruption of the MMAC1/PTEN gene by deletion or mutation is a frequent event in malignant melanoma. Cancer Res 1997;57(17):3660-3
  • Teng DH, Hu R, Lin H, et al. MMAC1/PTEN mutations in primary tumor specimens and tumor cell lines. Cancer Res 1997;57(23):5221-5
  • Chudnovsky Y, Khavari PA, Adams AE. Melanoma genetics and the development of rational therapeutics. J Clin Invest 2005;115(4):813-24
  • Diehl JA, Cheng M, Roussel MF, Sherr CJ. Glycogen synthase kinase-3beta regulates cyclin D1 proteolysis and subcellular localization. Genes Dev 1998;12(22):3499-511
  • Bedogni B, Welford SM, Cassarino DS, et al. The hypoxic microenvironment of the skin contributes to Akt-mediated melanocyte transformation. Cancer Cell 2005;8(6):443-54
  • Brazil DP, Park J, Hemmings BA. PKB binding proteins. Getting in on the Akt. Cell 2002;111(3):293-303
  • Stahl JM, Sharma A, Cheung M, et al. Deregulated Akt3 activity promotes development of malignant melanoma. Cancer Res 2004;64(19):7002-10
  • Krasilnikov M, Adler V, Fuchs SY, et al. Contribution of phosphatidylinositol 3-kinase to radiation resistance in human melanoma cells. Mol Carcinog 1999;24(1):64-9
  • Bedogni B, Welford SM, Kwan AC, et al. Inhibition of phosphatidylinositol-3-kinase and mitogen-activated protein kinase kinase 1/2 prevents melanoma development and promotes melanoma regression in the transgenic TPRas mouse model. Mol Cancer Ther 2006;5(12):3071-7
  • Smalley KS, Haass NK, Brafford PA, et al. Multiple signaling pathways must be targeted to overcome drug resistance in cell lines derived from melanoma metastases. Mol Cancer Ther 2006;5(5):1136-44
  • Tran MA, Gowda R, Sharma A, et al. Targeting V600EB-Raf and Akt3 using nanoliposomal-small interfering RNA inhibits cutaneous melanocytic lesion development. Cancer Res 2008;68(18):7638-49
  • Levy DS, Kahana JA, Kumar R. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines. Blood 2009;113(8):1723-9
  • Howes AL, Chiang GG, Lang ES, et al. The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures. Mol Cancer Ther 2007;6(9):2505-14
  • Reiling JH, Sabatini DM. Stress and mTORture signaling. Oncogene 2006;25(48):6373-83
  • Sarbassov DD, Ali SM, Kim DH, et al. Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton. Curr Biol 2004;14(14):1296-302
  • Guertin DA, Stevens DM, Thoreen CC, et al. Ablation in mice of the mTORC components raptor, rictor, or mLST8 reveals that mTORC2 is required for signaling to Akt-FOXO and PKCalpha, but not S6K1. Dev Cell 2006;11(6):859-71
  • Zeng Z, Sarbassov dos D, Samudio IJ, et al. Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AML. Blood 2007;109(8):3509-12
  • Karbowniczek M, Spittle CS, Morrison T, et al. mTOR is activated in the majority of malignant melanomas. J Invest Dermatol 2008;128(4):980-7
  • Molhoek KR, Brautigan DL, Slingluff CL. Synergistic inhibition of human melanoma proliferation by combination treatment with B-Raf inhibitor BAY43-9006 and mTOR inhibitor Rapamycin. J Transl Med 2005;3:39
  • Margolin K, Longmate J, Baratta T, et al. CCI-779 in metastatic melanoma: a phase II trial of the California cancer consortium. Cancer 2005;104(5):1045-8
  • O'Reilly KE, Rojo F, She QB, et al. mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res 2006;66(3):1500-8
  • Werzowa J, Cejka D, Fuereder T, et al. Suppression of mTOR complex 2-dependent AKT phosphorylation in melanoma cells by combined treatment with rapamycin and LY294002. Br J Dermatol 2008 [Epub ahead of print]
  • Lasithiotakis KG, Sinnberg TW, Schittek B, et al. Combined inhibition of MAPK and mTOR signaling inhibits growth, induces cell death, and abrogates invasive growth of melanoma cells. J Invest Dermatol 2008;128(8):2013-23
  • Verhaegen M, Bauer JA, Martin de la Vega C, et al. A novel BH3 mimetic reveals a mitogen-activated protein kinase-dependent mechanism of melanoma cell death controlled by p53 and reactive oxygen species. Cancer Res 2006;66(23):11348-59
  • Bruns CJ, Koehl GE, Guba M, et al. Rapamycin-induced endothelial cell death and tumor vessel thrombosis potentiate cytotoxic therapy against pancreatic cancer. Clin Cancer Res 2004;10(6):2109-19
  • Seeliger H, Guba M, Koehl GE, et al. Blockage of 2-deoxy-D-ribose-induced angiogenesis with rapamycin counteracts a thymidine phosphorylase-based escape mechanism available for colon cancer under 5-fluorouracil therapy. Clin Cancer Res 2004;10(5):1843-52
  • Beuvink I, Boulay A, Fumagalli S, et al. The mTOR inhibitor RAD001 sensitizes tumor cells to DNA-damaged induced apoptosis through inhibition of p21 translation. Cell 2005;120(6):747-59
  • Sinnberg T, Lasithiotakis K, Niessner H, et al. Inhibition of PI3K-AKT-mTOR signaling sensitizes melanoma cells to cisplatin and temozolomide. J Invest Dermatol 2008 [Epub ahead of print]
  • Hersey P. Apoptosis and melanoma: how new insights are effecting the development of new therapies for melanoma. Curr Opin Oncol 2006;18(2):189-96
  • Thallinger C, Poeppl W, Pratscher B, et al. CCI-779 plus cisplatin is highly effective against human melanoma in a SCID mouse xenotranplantation model. Pharmacology 2007;79(4):207-13
  • Thallinger C, Werzowa J, Poeppl W, et al. Comparison of a treatment strategy combining CCI-779 plus DTIC versus DTIC monotreatment in human melanoma in SCID mice. J Invest Dermatol 2007;127(10):2411-7
  • Lapidot T, Sirard C, Vormoor J, et al. A cell initiating human acute myeloid leukaemia after transplantation into SCID mice. Nature 1994;367(6464):645-8
  • Al-Hajj M, Wicha MS, Benito-Hernandez A, et al. Prospective identification of tumorigenic breast cancer cells. Proc Natl Acad Sci USA 2003;100(7):3983-8
  • Singh SK, Clarke ID, Terasaki M, et al. Identification of a cancer stem cell in human brain tumors. Cancer Res 2003;63(18):5821-8
  • Collins AT, Berry PA, Hyde C, et al. Prospective identification of tumorigenic prostate cancer stem cells. Cancer Res 2005;65(23):10946-51
  • Dalerba P, Dylla SJ, Park IK, et al. Phenotypic characterization of human colorectal cancer stem cells. Proc Natl Acad Sci USA 2007;104(24):10158-63
  • Schatton T, Murphy GF, Frank NY, et al. Identification of cells initiating human melanomas. Nature 2008;451(7176):345-9
  • Shmelkov SV, Butler JM, Hooper AT, et al. CD133 expression is not restricted to stem cells, and both CD133 and CD133 metastatic colon cancer cells initiate tumors. J Clin Invest 2008;118(6):2111-20
  • Fang D, Nguyen TK, Leishear K, et al. A tumorigenic subpopulation with stem cell properties in melanomas. Cancer Res 2005;65(20):9328-37
  • Monzani E, Facchetti F, Galmozzi E, et al. Melanoma contains CD133 and ABCG2 positive cells with enhanced tumourigenic potential. Eur J Cancer 2007;43(5):935-46
  • Quintana E, Shackleton M, Sabel MS, et al. Efficient tumour formation by single human melanoma cells. Nature 2008;456(7222):593-8
  • Smalley KS, Xiao M, Villanueva J, et al. CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations. Oncogene 2008: ePub Sep 15th
  • Hodi FS, Friedlander P, Corless CL, et al. Major response to imatinib mesylate in KIT-mutated melanoma. J Clin Oncol 2008;26(12):2046-51
  • Bedogni B, O'Neill MS, Welford SM, et al. Topical treatment with inhibitors of the phosphatidylinositol 3′-kinase/Akt and Raf/mitogen-activated protein kinase kinase/extracellular signal-regulated kinase pathways reduces melanoma development in severe combined immunodeficient mice. Cancer Res 2004;64(7):2552-60
  • Cragg MS, Jansen ES, Cook M, et al. Treatment of B-RAF mutant human tumor cells with a MEK inhibitor requires Bim and is enhanced by a BH3 mimetic. J Clin Invest 2008;118(11):3651-9
  • Carracedo A, Ma L, Teruya-Feldstein J, et al. Inhibition of mTORC1 leads to MAPK pathway activation through a PI3K-dependent feedback loop in human cancer. J Clin Invest 2008;118(9):3065-74
  • Sensi M, Nicolini G, Petti C, et al. Mutually exclusive NRASQ61R and BRAFV600E mutations at the single-cell level in the same human melanoma. Oncogene 2006;25(24):3357-64
  • Mellor HR, Ferguson DJ, Callaghan R. A model of quiescent tumour microregions for evaluating multicellular resistance to chemotherapeutic drugs. Br J Cancer 2005;93(3):302-9
  • Gascoigne KE, Taylor SS. Cancer cells display profound intra- and interline variation following prolonged exposure to antimitotic drugs. Cancer Cell 2008;14(2):111-22
  • Cohen AA, Geva-Zatorsky N, Eden E, et al. Dynamic proteomics of individual cancer cells in response to a drug. Science 2008;322(5907):1511-6
  • Ley TJ, Mardis ER, Ding L, et al. DNA sequencing of a cytogenetically normal acute myeloid leukaemia genome. Nature 2008;456(7218):66-72

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