Tailoring tyrosine kinase inhibitors to fit the lung cancer genome

Translational Oncology

Volumn 4, Issue 2, 2011, Pages 59-70

  Looyenga, Brendan D ^a   Cherni, Irene ^b   MacKeigan, Jeffrey P ^a   Weiss, Glen J ^b,c  

^a VAN ANDEL RESEARCH INSTITUTE   (United States)

^b TRANSLATIONAL GENOMICS RESEARCH INSTITUTE   (United States)

^c Virginia G Piper Cancer Center   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [1 (2,6 DICHLORO 3 FLUOROPHENYL)ETHOXY] 5 [1 (4 PIPERIDINYL) 1H PYRAZOL 4 YL] 2 PYRIDINYLAMINE; AFATINIB; ANTINEOPLASTIC AGENT; ARQ 197; AZD 4547; BGJ 398; BMS 754807; DOVITINIB; ERLOTINIB; FORETINIB; GEFITINIB; GSK 2256098; HISTONE DEACETYLASE INHIBITOR; IMATINIB; INTEDANIB; LAPATINIB; LESTAURTINIB; PAZOPANIB; PF 04554878; PF 299804; PHA 665257; PROTEIN TYROSINE KINASE INHIBITOR; SORAFENIB; SUNITINIB; UNCLASSIFIED DRUG; UNINDEXED DRUG; VANDETANIB; VATALANIB; XL 184; XL 228; XL 647;

ARTICLE; CANCER CLASSIFICATION; COPY NUMBER VARIATION; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG TARGETING; GENE AMPLIFICATION; GENE DOSAGE; GENE MUTATION; GENE SEQUENCE; GENOME; HUMAN; LUNG NON SMALL CELL CANCER; NONHUMAN; POINT MUTATION; SIGNAL TRANSDUCTION; TREATMENT RESPONSE;

EID: 79953653092     PISSN: None     EISSN: 19365233     Source Type: Journal    
DOI: 10.1593/tlo.10241     Document Type: Article

References (161)

1. ICGC (2010). International network of cancer genome projects. Nature 464, 993-998.
2. Beroukhim R, Mermel CH, Porter D, Wei G, Raychaudhuri S, Donovan J, Barretina J, Boehm JS, Dobson J, Urashima M, et al. (2010). The landscape of somatic copy-number alteration across human cancers. Nature 463, 899-905.
3. Ding L, Getz G, Wheeler DA, Mardis ER, McLellan MD, Cibulskis K, Sougnez C, Greulich H, Muzny DM, Morgan MB, et al. (2008). Somatic mutations affect key pathways in lung adenocarcinoma. Nature 455, 1069-1075.
4. Lee W, Jiang Z, Liu J, Haverty PM, Guan Y, Stinson J, Yue P, Zhang Y, Pant KP, Bhatt D, et al. (2010). The mutation spectrum revealed by paired genome sequences from a lung cancer patient. Nature 465, 473-477.
5. Weir BA, Woo MS, Getz G, Perner S, Ding L, Beroukhim R, Lin WM, Province MA, Kraja A, Johnson LA, et al. (2007). Characterizing the cancer genome in lung adenocarcinoma. Nature 450, 893-898.
6. Ding L, Ellis MJ, Li S, Larson DE, Chen K, Wallis JW, Harris CC, McLellan MD, Fulton RS, Fulton LL, et al. (2010). Genome remodelling in a basal-like breast cancer metastasis and xenograft. Nature 464, 999-1005.
7. Parsons DW, Jones S, Zhang X, Lin JC, Leary RJ, Angenendt P, Mankoo P, Carter H, Siu IM, Gallia GL, et al. (2008). An integrated genomic analysis of human glioblastoma multiforme. Science 321, 1807-1812.
8. Gazdar AF (2009). Personalized medicine and inhibition of EGFR signaling in lung cancer. N Engl J Med 361, 1018-1020.
9. Wakelee H, Loo BW Jr, Kernstine KH, Putnam JB Jr, Edelman MJ, Vokes EE, Schiller JH, Baas P, Saijo N, Adjei A, et al. (2009). Cooperative group research efforts in thoracic malignancies 2009: a review from the 10th Annual International Lung Cancer Congress. Clin Lung Cancer 10, 395-404.
10. Hutchinson L and DeVita VT Jr (2008). The era of personalized medicine: back to basics. Nat Clin Pract Oncol 5, 623.
11. Perez-Soler R (2009). Individualized therapy in non-small-cell lung cancer: future versus current clinical practice. Oncogene 28(suppl 1), S38-S45.
12. Herbst RS, Heymach JV, and Lippman SM (2008). Lung cancer. N Engl J Med 359, 1367-1380.
13. Bergh JC (1990). Gene amplification in human lung cancer. The myc family genes and other proto-oncogenes and growth factor genes. Am Rev Respir Dis 142, S20-S26.
14. Siegfried JM, Gillespie AT, Mera R, Casey TJ, Keohavong P, Testa JR, and Hunt JD (1997). Prognostic value of specific KRAS mutations in lung adenocarcinomas. Cancer Epidemiol Biomarkers Prev 6, 841-847.
15. Shiraishi M, Noguchi M, Shimosato Y, and Sekiya T (1989). Amplification of protooncogenes in surgical specimens of human lung carcinomas. Cancer Res 49, 6474-6479.
16. Blume-Jensen P and Hunter T (2001). Oncogenic kinase signalling. Nature 411, 355-365.
17. Lemmon MA and Schlessinger J (2010). Cell signaling by receptor tyrosine kinases. Cell 141, 1117-1134.
18. Vlahovic G and Crawford J (2003). Activation of tyrosine kinases in cancer. Oncologist 8, 531-538.
19. Natoli C, Perrucci B, Perrotti F, Falchi L, and Iacobelli S (2010). Tyrosine kinase inhibitors. Curr Cancer Drug Targets 10, 462-483.
20. Jonkers J and Berns A (2004). Oncogene addiction: sometimes a temporary slavery. Cancer Cell 6, 535-538.
21. Weinstein IB and Joe AK (2006). Mechanisms of disease: oncogene addiction- a rationale for molecular targeting in cancer therapy. Nat Clin Pract Oncol 3, 448-457.
22. Weinstein IB (2002). Cancer. Addiction to oncogenes-the Achilles heal of cancer. Science 297, 63-64.
23. Ren R (2005). Mechanisms of BCR-ABL in the pathogenesis of chronic myelogenous leukaemia. Nat Rev Cancer 5, 172-183.
24. Hudziak RM, Lewis GD, Winget M, Fendly BM, Shepard HM, and Ullrich A (1989). p185HER2 monoclonal antibody has antiproliferative effects in vitro and sensitizes human breast tumor cells to tumor necrosis factor. Mol Cell Biol 9, 1165-1172.
25. Shawver LK, Slamon D, and Ullrich A (2002). Smart drugs: tyrosine kinase inhibitors in cancer therapy. Cancer Cell 1, 117-123.
26. Schneider-Merck T and Trepel M (2010). Lapatinib. Recent Results Cancer Res 184, 45-59.
27. Sharma SV and Settleman J (2007). Oncogene addiction: setting the stage for molecularly targeted cancer therapy. Genes Dev 21, 3214-3231.
28. Engelman JA and Janne PA (2008). Mechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Clin Cancer Res 14, 2895-2899.
29. Xu AM and Huang PH (2010). Receptor tyrosine kinase coactivation networks in cancer. Cancer Res 70, 3857-3860.
30. Stewart DJ, Whitney SN, and Kurzrock R (2010). Equipoise lost: ethics, costs, and the regulation of cancer clinical research. J Clin Oncol 28, 2925-2935.
31. Selvaggi G and Scagliotti GV (2009). Histologic subtype in NSCLC: does it matter? Oncology (Williston Park) 23, 1133-1140.
32. Pao W, Wang TY, Riely GJ, Miller VA, Pan Q, Ladanyi M, Zakowski MF, Heelan RT, Kris MG, and Varmus HE (2005). KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med 2, e17.
33. Tam IY, Chung LP, Suen WS, Wang E, Wong MC, Ho KK, Lam WK, Chiu SW, Girard L, Minna JD, et al. (2006). Distinct epidermal growth factor receptor and KRAS mutation patterns in non-small cell lung cancer patients with different tobacco exposure and clinicopathologic features. Clin Cancer Res 12, 1647-1653.
34. Solomon B, Varella-Garcia M, and Camidge DR (2009). ALK gene rearrangements: a new therapeutic target in a molecularly defined subset of non-small cell lung cancer. J Thorac Oncol 4, 1450-1454.
35. Mao C, Qiu LX, Liao RY, Du FB, Ding H, Yang WC, Li J, and Chen Q (2009). KRAS mutations and resistance to EGFR-TKIs treatment in patients with non-small cell lung cancer: a meta-analysis of 22 studies. Lung Cancer 69, 272-278.
36. Young A, Lyons J, Miller AL, Phan VT, Alarcon IR, and McCormick F (2009). Ras signaling and therapies. Adv Cancer Res 102, 1-17.
37. Legrier ME, Yang CP, Yan HG, Lopez-Barcons L, Keller SM, Perez-Soler R, Horwitz SB, and McDaid HM (2007). Targeting protein translation in human non small cell lung cancer via combined MEK and mammalian target of rapamycin suppression. Cancer Res 67, 11300-11308.
38. Faivre S, Djelloul S, and Raymond E (2006). New paradigms in anticancer therapy: targeting multiple signaling pathways with kinase inhibitors. Semin Oncol 33, 407-420.
39. Walker K and Olson MF (2005). Targeting Ras and Rho GTPases as opportunities for cancer therapeutics. Curr Opin Genet Dev 15, 62-68.
40. American Cancer Society (2010). Cancer Facts & Figures, 2010. American Cancer Society, Atlanta, GA.
41. Jackman DM, Miller VA, Cioffredi LA, Yeap BY, Janne PA, Riely GJ, Ruiz MG, Giaccone G, Sequist LV, and Johnson BE (2009). Impact of epidermal growth factor receptor and KRAS mutations on clinical outcomes in previously untreated non-small cell lung cancer patients: results of an online tumor registry of clinical trials. Clin Cancer Res 15, 5267-5273.
42. Tsujino K, Kawaguchi T, Kubo A, Aono N, Nakao K, Koh Y, Tachibana K, Isa S, Takada M, and Kurata T (2009). Response rate is associated with prolonged survival in patients with advanced non-small cell lung cancer treated with gefitinib or erlotinib. J Thorac Oncol 4, 994-1001.
43. Fuster LM and Sandler AB (2004). Select clinical trials of erlotinib (OSI-774) in non-small-cell lung cancer with emphasis on phase III outcomes. Clin Lung Cancer 6(suppl 1), S24-S29.
44. Milano G, Spano JP, and Leyland-Jones B (2008). EGFR-targeting drugs in combination with cytotoxic agents: from bench to bedside, a contrasted reality. Br J Cancer 99, 1-5.
45. Rosell R, Taron M, Reguart N, Isla D, and Moran T (2006). Epidermal growth factor receptor activation: how exon 19 and 21 mutations changed our understanding of the pathway. Clin Cancer Res 12, 7222-7231.
46. Dahabreh IJ, Linardou H, Siannis F, Kosmidis P, Bafaloukos D, and Murray S (2010). Somatic EGFR mutation and gene copy gain as predictive biomarkers for response to tyrosine kinase inhibitors in non-small cell lung cancer. Clin Cancer Res 16, 291-303.
47. Bell DW, Lynch TJ, Haserlat SM, Harris PL, Okimoto RA, Brannigan BW, Sgroi DC, Muir B, Riemenschneider MJ, Iacona RB, et al. (2005). Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials. J Clin Oncol 23, 8081-8092.
48. Wheeler DL, Dunn EF, and Harari PM (2010). Understanding resistance to EGFR inhibitors-impact on future treatment strategies. Nat Rev Clin Oncol 7, 493-507.
49. Jackman D, Pao W, Riely GJ, Engelman JA, Kris MG, Janne PA, Lynch T, Johnson BE, and Miller VA (2010). Clinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer. J Clin Oncol 28, 357-360.
50. La Rosee P and Hochhaus A (2010). Molecular pathogenesis of tyrosine kinase resistance in chronic myeloid leukemia. Curr Opin Hematol 17, 91-96.
51. Gorre ME, Mohammed M, Ellwood K, Hsu N, Paquette R, Rao PN, and Sawyers CL (2001). Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 293, 876-880.
52. Kobayashi S, Boggon TJ, Dayaram T, Janne PA, Kocher O, Meyerson M, Johnson BE, Eck MJ, Tenen DG, and Halmos B (2005). EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 352, 786-792.
53. Pao W, Miller VA, Politi KA, Riely GJ, Somwar R, Zakowski MF, Kris MG, and Varmus H (2005). Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med 2, e73.
54. Bean J, Riely GJ, Balak M, Marks JL, Ladanyi M, Miller VA, and Pao W (2008). Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma. Clin Cancer Res 14, 7519-7525.
55. Stamos J, Sliwkowski MX, and Eigenbrot C (2002). Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4- anilinoquinazoline inhibitor. J Biol Chem 277, 46265-46272.
56. Kwak EL, Sordella R, Bell DW, Godin-Heymann N, Okimoto RA, Brannigan BW, Harris PL, Driscoll DR, Fidias P, Lynch TJ, et al. (2005). Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci USA 102, 7665-7670.
57. Sos ML, Rode HB, Heynck S, Peifer M, Fischer F, Kluter S, Pawar VG, Reuter C, Heuckmann JM, Weiss J, et al. (2010). Chemogenomic profiling provides insights into the limited activity of irreversible EGFR inhibitors in tumor cells expressing the T790M EGFR resistance mutation. Cancer Res 70, 868-874.
58. Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, et al. (2009). Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462, 1070-1074.
59. Engelman JA, Zejnullahu K, Mitsudomi T, Song Y, Hyland C, Park JO, Lindeman N, Gale CM, Zhao X, Christensen J, et al. (2007). MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316, 1039-1043.
60. Turke AB, Zejnullahu K, Wu YL, Song Y, Dias Santagata D, Lifshits E, Toschi L, Rogers A, Mok T, Sequist L, et al. (2010). Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell 17, 77-88.
61. Guix M, Faber AC, Wang SE, Olivares MG, Song Y, Qu S, Rinehart C, Seidel B, Yee D, Arteaga CL, et al. (2008). Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins. J Clin Invest 118, 2609-2619.
62. Dziadziuszko R, Merrick DT, Witta SE, Mendoza AD, Szostakiewicz B, Szymanowska A, Rzyman W, Dziadziuszko K, Jassem J, Bunn PA Jr, et al. (2010). Insulin-like growth factor receptor 1 (IGF1R) gene copy number is associated with survival in operable non-small-cell lung cancer: a comparison between IGF1R fluorescent in situ hybridization, protein expression, and mRNA expression. J Clin Oncol 28, 2174-2180.
63. Kono SA, Marshall ME, Ware KE, and Heasley LE (2009). The fibroblast growth factor receptor signaling pathway as a mediator of intrinsic resistance to EGFRspecific tyrosine kinase inhibitors in non-small cell lung cancer. Drug Resist Updat 12, 95-102.
64. Thomson S, Petti F, Sujka-Kwok I, Epstein D, and Haley JD (2008). Kinase switching in mesenchymal-like non-small cell lung cancer lines contributes to EGFR inhibitor resistance through pathway redundancy. Clin Exp Metastasis 25, 843-854.
65. Raponi M, Winkler H, and Dracopoli NC (2008). KRAS mutations predict response to EGFR inhibitors. Curr Opin Pharmacol 8, 413-418.
66. Amler LC, Goddard AD, and Hillan KJ (2005). Predicting clinical benefit in non-small-cell lung cancer patients treated with epidermal growth factor tyrosine kinase inhibitors. Cold Spring Harb Symp Quant Biol 70, 483-488.
67. Sharma SV, Lee DY, Li B, Quinlan MP, Takahashi F, Maheswaran S, McDermott U, Azizian N, Zou L, Fischbach MA, et al. (2010). A chromatin-mediated reversible drug-tolerant state in cancer cell subpopulations. Cell 141, 69-80.
68. Glinsky GV (2008). "Stemness" genomics law governs clinical behavior of human cancer: implications for decision making in disease management. J Clin Oncol 26, 2846-2853.
69. Visvader JE and Lindeman GJ (2008). Cancer stem cells in solid tumours: accumulating evidence and unresolved questions. Nat Rev Cancer 8, 755-768.
70. Dean M, Fojo T, and Bates S (2005). Tumour stem cells and drug resistance. Nat Rev Cancer 5, 275-284.
71. Elrick LJ, Jorgensen HG, Mountford JC, and Holyoake TL (2005). Punish the parent not the progeny. Blood 105, 1862-1866.
72. Roesch A, Fukunaga-Kalabis M, Schmidt EC, Zabierowski SE, Brafford PA, Vultur A, Basu D, Gimotty P, Vogt T, and Herlyn M (2010). A temporarily distinct subpopulation of slow-cycling melanoma cells is required for continuous tumor growth. Cell 141, 583-594.
73. Birchmeier C, Birchmeier W, Gherardi E, and Vande Woude GF (2003). Met, metastasis, motility and more. Nat Rev Mol Cell Biol 4, 915-925.
74. Stellrecht CM and Gandhi V (2009). MET receptor tyrosine kinase as a therapeutic anticancer target. Cancer Lett 280, 1-14.
75. Eder JP, Vande Woude GF, Boerner SA, and LoRusso PM (2009). Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin Cancer Res 15, 2207-2214.
76. McDermott U, Pusapati RV, Christensen JG, Gray NS, and Settleman J (2010). Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res 70, 1625-1634.
77. Chiarle R, Voena C, Ambrogio C, Piva R, and Inghirami G (2008). The anaplastic lymphoma kinase in the pathogenesis of cancer. Nat Rev Cancer 8, 11-23.
78. Mosse YP, Laudenslager M, Longo L, Cole KA, Wood A, Attiyeh EF, Laquaglia MJ, Sennett R, Lynch JE, Perri P, et al. (2008). Identification of ALK as a major familial neuroblastoma predisposition gene. Nature 455, 930-935.
79. Cheng M and Ott GR (2010). Anaplastic lymphoma kinase as a therapeutic target in anaplastic large cell lymphoma, non-small cell lung cancer and neuroblastoma. Anticancer Agents Med Chem 10, 236-249.
80. Soda M, Choi YL, Enomoto M, Takada S, Yamashita Y, Ishikawa S, Fujiwara S, Watanabe H,KurashinaK,HatanakaH, et al. (2007). Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer. Nature 448, 561-566.
81. McDermott U, Iafrate AJ, Gray NS, Shioda T, Classon M, Maheswaran S, Zhou W, Choi HG, Smith SL, Dowell L, et al. (2008). Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res 68, 3389-3395.
82. Shaw AT, Yeap BY, Mino-Kenudson M, Digumarthy SR, Costa DB, Heist RS, Solomon B, Stubbs H, Admane S, McDermott U, et al. (2009). Clinical features and outcome of patients with non-small-cell lung cancer who harbor EML4- ALK. J Clin Oncol 27, 4247-4253.
83. Sasaki T, Rodig SJ, Chirieac LR, and Janne PA (2010). The biology and treatment of EML4-ALK non-small cell lung cancer. Eur J Cancer 46, 1773-1780.
84. Yamazaki S, Skaptason J, Romero D, Lee JH, Zou HY, Christensen JG, Koup JR, Smith BJ, and Koudriakova T (2008). Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse models. Drug Metab Dispos 36, 1267-1274.
85. Koivunen JP, Mermel C, Zejnullahu K, Murphy C, Lifshits E, Holmes AJ, Choi HG, Kim J, Chiang D, Thomas R, et al. (2008). EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res 14, 4275-4283.
86. Bang Y, Kwak EL, Shaw AT, Camidge DR, Iafrate AJ, Maki RG, Solomon BJ, Ou SI, Salgia R, and Clark JW (2010). Clinical activity of the oral ALK inhibitor PF-02341066 in ALK-positive with non-small cell lung cancer (NSCLC). In ASCO Annual '10 Meeting; Chicago, IL. Abstract No. 3.
87. Pasquale EB (2010). Eph receptors and ephrins in cancer: bidirectional signalling and beyond. Nat Rev Cancer 10, 165-180.
88. Antoniu SA and Kolb MR (2010). Intedanib, a triple kinase inhibitor of VEGFR, FGFR and PDGFR for the treatment of cancer and idiopathic pulmonary fibrosis. IDrugs 13, 332-345.
89. Kim DW, Lu B, and Hallahan DE (2004). Receptor tyrosine kinase inhibitors as anti-angiogenic agents. Curr Opin Investig Drugs 5, 597-604.
90. Heath VL and Bicknell R (2009). Anticancer strategies involving the vasculature. Nat Rev Clin Oncol 6, 395-404.
91. Marek L, Ware KE, Fritzsche A, Hercule P, Helton WR, Smith JE, McDermott LA, Coldren CD, Nemenoff RA, Merrick DT, et al. (2009). Fibroblast growth factor (FGF) and FGF receptor-mediated autocrine signaling in non-small-cell lung cancer cells. Mol Pharmacol 75, 196-207.
92. Berger W, Setinek U, Mohr T, Kindas-Mugge I, Vetterlein M, Dekan G, Eckersberger F, Caldas C, and Micksche M (1999). Evidence for a role of FGF-2 and FGF receptors in the proliferation of non-small cell lung cancer cells. Int J Cancer 83, 415-423.
93. Angevin E, Lin C, Pande AU, Lopez JA, Gschwend J, Harzstark AL, Shi M, Anak O, and Escudier BJ (2010). A phase I/II study of dovitinib (TKI258), a FGFR and VEGFR inhibitor, in patients (pts) with advanced or metastatic renal cell cancer: phase I results. In ASCO Annual '10 Meeting; Chicago, IL. Abstract No. 3057.
94. Lee CB and Socinski MA (2007). Vascular endothelial growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer: a review of recent clinical trials. Rev Recent Clin Trials 2, 117-120.
95. Ivy SP, Wick JY, and Kaufman BM (2009). An overview of small-molecule inhibitors of VEGFR signaling. Nat Rev Clin Oncol 6, 569-579.
96. Atkins M, Jones CA, and Kirkpatrick P (2006). Sunitinib maleate. Nat Rev Drug Discov 5, 279-280.
97. Wilhelm S, Carter C, Lynch M, Lowinger T, Dumas J, Smith RA, Schwartz B, Simantov R, and Kelley S (2006). Discovery and development of sorafenib: a multikinase inhibitor for treating cancer. Nat Rev Drug Discov 5, 835-844.
98. Lind JS, Dingemans AM, Groen HJ, Thunnissen FB, Bekers O, Heideman DA, Honeywell RJ, Giovannetti E, Peters GJ, Postmus PE, et al. (2010). A multicenter phase II study of erlotinib and sorafenib in chemotherapy-naive patients with advanced non-small cell lung cancer. Clin Cancer Res 16, 3078-3087.
99. Takezawa K, Okamoto I, Yonesaka K, Hatashita E, Yamada Y, Fukuoka M, and Nakagawa K (2009). Sorafenib inhibits non-small cell lung cancer cell growth by targeting B-RAF in KRAS wild-type cells and C-RAF in KRAS mutant cells. Cancer Res 69, 6515-6521.
100. Kim ES, Herbst R, Lee JJ, Blumenschein GR, Tsao A, Alden CM, Tang X, Liu S, Stewart DJ, Heymach JV, et al. (2010). The BATTLE trial (Biomarker-integrated Approaches of Targeted Therapy for Lung Cancer Elimination): personlazing therapy for lung cancer. In 2010 American Association for Cancer Research Annual Meeting; Washington, DC. Abstract No. LB-1.
101. Scagliotti G and Govindan R (2010). Targeting angiogenesis with multitargeted tyrosine kinase inhibitors in the treatment of non-small cell lung cancer. Oncologist 15, 436-446.
102. Bukowski RM, Yasothan U, and Kirkpatrick P (2010). Pazopanib. Nat Rev Drug Discov 9, 17-18.
103. Jain RK, Duda DG, Clark JW, and Loeffler JS (2006). Lessons from phase III clinical trials on anti-VEGF therapy for cancer. Nat Clin Pract Oncol 3, 24-40.
104. Heymach JV, Paz-Ares L, De Braud F, Sebastian M, Stewart DJ, Eberhardt WE, Ranade AA, Cohen G, Trigo JM, Sandler AB, et al. (2008). Randomized phase II study of vandetanib alone or with paclitaxel and carboplatin as first-line treatment for advanced non-small-cell lung cancer. J ClinOncol 26, 5407-5415.
105. Natale RB, Bodkin D, Govindan R, Sleckman BG, Rizvi NA, Capo A, Germonpre P, Eberhardt WE, Stockman PK, Kennedy SJ, et al. (2009). Vandetanib versus gefitinib in patients with advanced non-small-cell lung cancer: results from a two-part, double-blind, randomized phase II study. J Clin Oncol 27, 2523-2529.
106. Eder JP, Shapiro GI, Appleman LJ, Zhu AX, Miles D, Keer H, Cancilla B, Chu F, Hitchcock-Bryan S, Sherman L, et al. (2010). A phase I study of foretinib, a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2. Clin Cancer Res 16, 3507-3516.
107. Byers LA and Heymach JV (2007). Dual targeting of the vascular endothelial growth factor and epidermal growth factor receptor pathways: rationale and clinical applications for non-small-cell lung cancer. Clin Lung Cancer 8(suppl 2), S79-S85.
108. Vlahovic G, Rabbani ZN, Herndon JE II, Dewhirst MW, and Vujaskovic Z (2006). Treatment with imatinib in NSCLC is associated with decrease of phosphorylated PDGFR-β and VEGF expression, decrease in interstitial fluid pressure and improvement of oxygenation. Br J Cancer 95, 1013-1019.
109. Besse B and Soria JC (2008). A randomized, double-blind, placebo-controlled phase II-III multi-centre study to evaluate the effect of adjuvant pazopanib (GW786034) versus placebo on post-surgical disease-free survival in patients with stage I non small cell lung cancer and tumor size equal or inferior to 5 cm. First Received: October 17, 2008. Last Updated: April 28, 2010. Available at: http://www.clinicaltrials.gov/ct2/show/NCT00775307?term=adjuvant+lung+cancer+pazopanib&rank=1.
110. Huang D, Ding Y, Zhou M, Rini BI, Petillo D, Qian CN, Kahnoski R, Futreal PA, Furge KA, and Teh BT (2010). Interleukin-8 mediates resistance to antiangiogenic agent sunitinib in renal cell carcinoma. Cancer Res 70, 1063-1071.
111. Koch AE, Polverini PJ, Kunkel SL, Harlow LA, DiPietro LA, Elner VM, Elner SG, and Strieter RM (1992). Interleukin-8 as a macrophage-derived mediator of angiogenesis. Science 258, 1798-1801.
112. Strieter RM, Belperio JA, Burdick MD, Sharma S, Dubinett SM, and Keane MP (2004). CXC chemokines: angiogenesis, immunoangiostasis, and metastases in lung cancer. Ann N Y Acad Sci 1028, 351-360.
113. Hanrahan EO, Lin HY, Kim ES, Yan S, Du DZ, McKee KS, Tran HT, Lee JJ, Ryan AJ, Langmuir P, et al. (2010). Distinct patterns of cytokine and angiogenic factor modulation and markers of benefit for vandetanib and/or chemotherapy in patients with non-small-cell lung cancer. J Clin Oncol 28, 193-201.
114. Thiery JP, Acloque H, Huang RY, and Nieto MA (2009). Epithelial-mesenchymal transitions in development and disease. Cell 139, 871-890.
115. Singh A and Settleman J (2010). EMT, cancer stem cells and drug resistance: an emerging axis of evil in the war on cancer. Oncogene 29, 4741-4751.
116. Hammers HJ, Verheul HM, Salumbides B, Sharma R, Rudek M, Jaspers J, Shah P, Ellis L, Shen L, Paesante S, et al. (2010). Reversible epithelial to mesenchymal transition and acquired resistance to sunitinib in patients with renal cell carcinoma: evidence from a xenograft study. Mol Cancer Ther 9, 1525-1535.
117. Barr S, Thomson S, Buck E, Russo S, Petti F, Sujka-Kwok I, Eyzaguirre A, Rosenfeld-Franklin M, Gibson NW, Miglarese M, et al. (2008). Bypassing cellular EGF receptor dependence through epithelial-to-mesenchymal-like transitions. Clin Exp Metastasis 25, 685-693.
118. Witta S, Konduri K, and Raju J (2008). A randomized, placebo-controlled, double-blind, multicenter phase 2 study with a lead in phase of erlotinib with or without SNDX-275 in patients with non-small cell lung carcinoma after failure in up to two prior chemotherapeutic regimens for advanced disease. First Received: January 25, 2008. Last Updated: February 2, 2010. Available at: http://clinicaltrials.gov/ct2/show/NCT00602030?term=MS-275&rank=2.
119. Spector DH, Varmus HE, and Bishop JM (1978). Nucleotide sequences related to the transforming gene of avian sarcoma virus are present in DNA of uninfected vertebrates. Proc Natl Acad Sci USA 75, 4102-4106.
120. Oppermann H, Levinson AD, Varmus HE, Levintow L, and Bishop JM (1979). Uninfected vertebrate cells contain a protein that is closely related to the product of the avian sarcoma virus transforming gene (src). Proc Natl Acad Sci USA 76, 1804-1808.
121. Kim LC, Song L, and Haura EB (2009). Src kinases as therapeutic targets for cancer. Nat Rev Clin Oncol 6, 587-595.
122. Elsberger B, Stewart B, Tatarov O, and Edwards J (2010). Is Src a viable target for treating solid tumours? Curr Cancer Drug Targets 10, 683-694.
123. Zhang J, Kalyankrishna S, Wislez M, Thilaganathan N, Saigal B, Wei W, Ma L, Wistuba II, Johnson FM, and Kurie JM (2007). SRC-family kinases are activated in non-small cell lung cancer and promote the survival of epidermal growth factor receptor-dependent cell lines. Am J Pathol 170, 366-376.
124. Song L, Morris M, Bagui T, Lee FY, Jove R, and Haura EB (2006). Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res 66, 5542-5548.
125. Schenone S, Brullo C, Musumeci F, and Botta M (2010). Novel dual Src/Abl inhibitors for hematologic and solid malignancies. Expert Opin Investig Drugs 19, 931-945.
126. Johnson FM, Saigal B, Talpaz M, and Donato NJ (2005). Dasatinib (BMS- 354825) tyrosine kinase inhibitor suppresses invasion and induces cell cycle arrest and apoptosis of head and neck squamous cell carcinoma and non-small cell lung cancer cells. Clin Cancer Res 11, 6924-6932.
127. Haura EB, Tanvetyanon T, Chiappori A, Williams C, Simon G, Antonia S, Gray J, Litschauer S, Tetteh L, Neuger A, et al. (2010). Phase I/II study of the Src inhibitor dasatinib in combination with erlotinib in advanced non-small-cell lung cancer. J Clin Oncol 28, 1387-1394.
128. Yoshida T, Okamoto I, Okamoto W, Hatashita E, Yamada Y, Kuwata K, Nishio K, Fukuoka M, Janne PA, and Nakagawa K (2010). Effects of Src inhibitors on cell growth and epidermal growth factor receptor and METsignaling in gefitinibresistant non-small cell lung cancer cells with acquired MET amplification. Cancer Sci 101, 167-172.
129. Mitra SK and Schlaepfer DD (2006). Integrin-regulated FAK-Src signaling in normal and cancer cells. Curr Opin Cell Biol 18, 516-523.
130. Schwock J, Dhani N, and Hedley DW (2010). Targeting focal adhesion kinase signaling in tumor growth and metastasis. Expert Opin Ther Targets 14, 77-94.
131. Meng XN, Jin Y, Yu Y, Bai J, Liu GY, Zhu J, Zhao YZ, Wang Z, Chen F, Lee KY, et al. (2009). Characterisation of fibronectin-mediated FAK signalling pathways in lung cancer cell migration and invasion. Br J Cancer 101, 327-334.
132. Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, et al. (2008). Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res 68, 1935-1944.
133. Wendt MK and Schiemann WP (2009). Therapeutic targeting of the focal adhesion complex prevents oncogenic TGF-β signaling and metastasis. Breast Cancer Res 11, R68.
134. Yu H, Pardoll D, and Jove R (2009). STATs in cancer inflammation and immunity: a leading role for STAT3. Nat Rev Cancer 9, 798-809.
135. Levine RL, Pardanani A, Tefferi A, and Gilliland DG (2007). Role of JAK2 in the pathogenesis and therapy of myeloproliferative disorders. Nat Rev Cancer 7, 673-683.
136. Cortas T, Eisenberg R, Fu P, Kern J, Patrick L, and Dowlati A (2007). Activation state EGFR and STAT-3 as prognostic markers in resected non-small cell lung cancer. Lung Cancer 55, 349-355.
137. Wu HY, Tseng VS, Chen LC, Chang HY, Chuang IC, Tsay YG, and Liao PC (2010). Identification of tyrosine-phosphorylated proteins associated with lung cancer metastasis using label-free quantitative analyses. J Proteome Res 9, 4102-4112.
138. He B, You L, Uematsu K, Zang K, Xu Z, Lee AY, Costello JF, McCormick F, and Jablons DM (2003). SOCS-3 is frequently silenced by hypermethylation and suppresses cell growth in human lung cancer. Proc Natl Acad SciUSA 100, 14133-14138.
139. Baltayiannis G, Baltayiannis N, and Tsianos EV (2008). Suppressors of cytokine signaling as tumor repressors. Silencing of SOCS3 facilitates tumor formation and growth in lung and liver. J BUON 13, 263-265.
140. Veeriah S, Brennan C, Meng S, Singh B, Fagin JA, Solit DB, Paty PB, Rohle D, Vivanco I, Chmielecki J, et al. (2009). The tyrosine phosphatase PTPRD is a tumor suppressor that is frequently inactivated and mutated in glioblastoma and other human cancers. Proc Natl Acad Sci USA 106, 9435-9440.
141. Lasho TL, Tefferi A, Hood JD, Verstovsek S, Gilliland DG, and Pardanani A (2008). TG101348, a JAK2-selective antagonist, inhibits primary hematopoietic cells derived from myeloproliferative disorder patients with JAK2V617F, MPLW515K or JAK2 exon 12 mutations as well as mutation negative patients. Leukemia 22, 1790-1792.
142. Pardanani A, Hood J, Lasho T, Levine RL, Martin MB, Noronha G, Finke C, Mak CC, Mesa R, Zhu H, et al. (2007). TG101209, a small molecule JAK2- selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia 21, 1658-1668.
143. Verstovsek S (2009). Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program 1, 636-642.
144. Wernig G, Kharas MG, Okabe R, Moore SA, Leeman DS, Cullen DE, Gozo M, McDowell EP, Levine RL, Doukas J, et al. (2008). Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617Finduced polycythemia vera. Cancer Cell 13, 311-320.
145. Janku F, Stewart DJ, and Kurzrock R (2010). Targeted therapy in non-smallcell lung cancer-is it becoming a reality? Nat Rev Clin Oncol 7, 401-414.
146. Janne PA (2008). Challenges of detecting EGFR T790M in gefitinib/erlotinib- resistant tumours. Lung Cancer 60(suppl 2), S3-S9.
147. Menendez-Arias L (2010). Molecular basis of human immunodeficiency virus drug resistance: an update. Antiviral Res 85, 210-231.
148. Ren J and Stammers DK (2008). Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIVreverse transcriptase. Virus Res 134, 157-170.
149. Naumov GN, Nilsson MB, Cascone T, Briggs A, Straume O, Akslen LA, Lifshits E, Byers LA, Xu L,Wu HK, et al. (2009). Combined vascular endothelial growth factor receptor and epidermal growth factor receptor (EGFR) blockade inhibits tumor growth in xenograft models of EGFR inhibitor resistance. Clin Cancer Res 15, 3484-3494.
150. Knight ZA and Shokat KM (2005). Features of selective kinase inhibitors. Chem Biol 12, 621-637.
151. Knight ZA, Lin H, and Shokat KM (2010). Targeting the cancer kinome through polypharmacology. Nat Rev Cancer 10, 130-137.
152. Yagui-Beltran A, He B, Raz D, Kim J, and Jablons DM (2006). Novel therapies targeting signaling pathways in lung cancer. Thorac Surg Clin 16, 379-396, vi.
153. Zhang Q, Feng W, Zhou H, and Yan B (2009). Advances in preclinical small molecules for the treatment of NSCLC. Expert Opin Ther Pat 19, 731-751.
154. Herbst RS, Prager D, Hermann R, Fehrenbacher L, Johnson BE, Sandler A, Kris MG, Tran HT, Klein P, Li X, et al. (2005). TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. J Clin Oncol 23, 5892-5899.
155. Herbst RS, Sun Y, Eberhardt WE, Germonpre P, Saijo N, Zhou C, Wang J, Li L, Kabbinavar F, Ichinose Y, et al. (2010). Vandetanib plus docetaxel versus docetaxel as second-line treatment for patients with advanced non-small-cell lung cancer (ZODIAC): a double-blind, randomised, phase 3 trial. Lancet Oncol 11, 619-626.
156. Ready N, Janne PA, Bogart J, Dipetrillo T, Garst J, Graziano S, Gu L, Wang X, Green MR, and Vokes EE (2010). Chemoradiotherapy and gefitinib in stage III non-small cell lung cancer with epidermal growth factor receptor and KRAS mutation analysis: cancer and leukemia group B (CALEB) 30106, a CALGBstratified phase II trial. J Thorac Oncol 5, 1382-1390.
157. Scagliotti G, Novello S, von Pawel J, Reck M, Pereira JR, Thomas M, Abrao Miziara JE, Balint B, De Marinis F, Keller A, et al. (2010). Phase III study of carboplatin and paclitaxel alone or with sorafenib in advanced non-small-cell lung cancer. J Clin Oncol 28, 1835-1842.
158. Kelly K, Chansky K, Gaspar LE, Albain KS, Jett J, Ung YC, Lau DH, Crowley JJ, and Gandara DR (2008). Phase III trial of maintenance gefitinib or placebo after concurrent chemoradiotherapy and docetaxel consolidation in inoperable stage III non-small-cell lung cancer: SWOG S0023. J Clin Oncol 26, 2450-2456.
159. Okamoto I, Takahashi T, Okamoto H, Nakagawa K, Watanabe K, Nakamatsu K, Nishimura Y, Fukuoka M, and Yamamoto N (2010). Single-agent gefitinib with concurrent radiotherapy for locally advanced non-small cell lung cancer harboring mutations of the epidermal growth factor receptor. Lung Cancer. Epub ahead of print.
160. Baselga J (2004). Combining the anti-EGFR agent gefitinib with chemotherapy in non-small-cell lung cancer: how do we go from INTACT to impact? J Clin Oncol 22, 759-761.
161. John T, Liu G, and Tsao MS (2009). Overview of molecular testing in non- small-cell lung cancer: mutational analysis, gene copy number, protein expression and other biomarkers of EGFR for the prediction of response to tyrosine kinase inhibitors. Oncogene 28(suppl 1), S14-S23.