Resistance to cancer treatment: The role of somatic genetic events and the challenges for targeted therapies

Frontiers in Pharmacology

Volumn OCT, Issue , 2011, Pages

  Batist, Gerald ^a,b,c   Wu, Jian Hui ^a,b,c   Spatz, Alan ^a,b,c   Miller, Wilson H ^a,b,c   Cocolakis, Eftihia ^a   Rousseau, Caroline ^c   Diaz, Zuanel ^c   Ferrario, Cristiano ^a,b,c   Basik, Mark ^a,b,c  

^a MCGILL UNIVERSITY   (Canada)

^b MCGILL UNIVERSITY   (Canada)

^c Quebec Consortium de Recherche en Oncologie Clinique   (Canada)

Author keywords

BCR Abl; Cancer; EML4 ALK; Somatic genetic events

Indexed keywords

ABIRATERONE; AG14361; B RAF KINASE INHIBITOR; BICALUTAMIDE; CETUXIMAB; CHIR 265; CISPLATIN; CRIZOTINIB; DOXORUBICIN; ERLOTINIB; GEFITINIB; GSK2118236; HYDROXYFLUTAMIDE; IMATINIB; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE INHIBITOR; NILUTAMIDE; OR5185426; PANITUMUMAB; TRASTUZUMAB; UNCLASSIFIED DRUG; VEMURAFENIB; XL 281;

ALK GENE; ARTICLE; BREAST CANCER; CANCER CELL; CANCER GENETICS; CANCER RESISTANCE; CANCER THERAPY; CASTRATION RESISTANT PROSTATE CANCER; CELL SURVIVAL; COLORECTAL CANCER; DETOXIFICATION; DNA REPAIR; DRUG MECHANISM; DRUG RESPONSE; EML4 GENE; ERBB2 GENE; GENE; GENE FUSION; HEAD AND NECK CANCER; HUMAN; LOSS OF FUNCTION MUTATION; LUNG NON SMALL CELL CANCER; MELANOMA; METASTATIC MELANOMA; MYELOID LEUKEMIA; NRAS GENE; OVARY CARCINOMA; PANCREAS CANCER; PROSTATE CANCER; SOMATIC MUTATION; STOMACH CARCINOMA;

EID: 84859265187     PISSN: None     EISSN: 16639812     Source Type: Journal    
DOI: 10.3389/fphar.2011.00059     Document Type: Article

References (65)

1. Agoulnik, I. U., and Weigel, N. L. (2006). Androgen receptor action in hormone-dependent and recurrent prostate cancer. J. Cell. Biochem. 99, 362-372.
2. Balk, S. P. (2002). Androgen receptor as a target in androgen-independent prostate cancer. Urology 60,132-138.
3. Bartsch, R., Wenzel, C., Altorjai, G., Pluschnig, U., Rudas, M., Mader, R. M., Gnant, M., Zielinski, C. C., and Steger, G. G. (2007). Capecitabine and trastuzumab in heavily pretreated metastatic breast cancer. J. Clin. Oncol. 25, 3853-3858.
4. Baselga, J., and Mendelsohn, J. (1997). Type I receptor tyrosine kinases as targets for therapy in breast cancer. J. Mammary Gland Biol. Neoplasia 2, 165-174.
5. Batist, G., Kavan, P., Orain, M., Camlioglu, E., Aguilar-Mahecha, A., Basik, M., Rousseau, C., Gagnon-Kugler, T., Spatz, A., and Têtu, B. (2010). "A biopsy-driven and bio-marker discovery clinical trial in metastatic colorectal cancer led by a new Quebec-wide translational research network, to identify signatures of clinical resistance," in ESMO, Milan.
6. Berg, M., Danielsen, S. A., Ahlquist, T., Merok, M. A., Ågesen, T. H., Vatn, M. H., Mala, T., Sjo, O. H., Bakka, A., Moberg, I., Fetveit, T., Mathisen, Ø., Husby, A., Sandvik, O., Nes-bakken, A., Thiis-Evensen, E., and Lothe, R. A. (2010). DNA sequence profiles of the colorectal cancer critical gene set KRAS-BRAF-PIK3CA-PTEN-TP53 related to age at disease onset. PLoS ONE 5, e13978. doi:10.1371/journal.pone.0013978
7. Chang, C. Y., Walther, P. J., and McDonnell, D. P. (2001). Glucocorticoids manifest androgenic activity in a cell line derived from a metastatic prostate cancer. Cancer Res. 61, 8712-8717.
8. Chapman, P. B., Hauschild, A., Robert, C., Haanen, J. B., Ascierto, P., Larkin, J., Dummer, R., Garbe, C., Testori, A., Maio, M., Hogg, D., Lorigan, P., Lebbe, C., Jouary, T., Schaden-dorf, D., Ribas, A., O'Day, S. J., Sos-man, J. A., Kirkwood, J. M., Egger-mont, A. M., Dreno, B., Nolop, K., Li, J., Nelson, B., Hou, J., Lee, R. J., Flaherty, K. T., McArthur, A. G., and BRIM-3 Study Group. (2011). Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation. N. Engl. J. Med. 364, 2507-2516.
9. Choi, Y. L., Soda, M., Yamashita, Y., Ueno, T., Takashima, J., Nakajima, T., Yatabe, Y., Takeuchi, K., Hamada, T., Haruta, H., Ishikawa, Y., Kimura, H., Mitsudomi, T., Tanio, Y., and Mano, H. (2010). ALK Lung Cancer Study Group. EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors. N. Engl. J. Med. 363, 1734-1739.
10. Christodoulou, C., Kostopoulos, I., Kalofonos, H. P., Lianos, E., Bobos, M., Briasoulis, E., Gogas, H., Razis, E., Skarlos, D. V., Fountzilas, G., and Study of the Hellenic Cooperative Oncology Group. (2009). Trastuzumab combined with pegylated liposomal doxorubicin in patients with metastatic breast cancer. phase II Study of the Hellenic Cooperative Oncology Group (HeCOG) with biomarker evaluation. Oncology 76, 275-285.
11. Corcoran, R. B., Dias-Santagata, D., Bergethon, K., Iafrate, A. J., Settle-man, J., and Engelman, J. A. (2010). BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutation. Sci. Signal. 3, ra84.
12. Culig, Z., Klocker, H., Bartsch, G., and Hobisch,A. (2002). Androgen receptors in prostate cancer. Endocr. Relat. Cancer 9, 155-170.
13. Davies, H., Bignell, G. R., Cox, C., Stephens, P., Edkins, S., Clegg, S., Teague, J., Woffendin, H., Garnett, M. J., Bottomley, W., Davis, N., Dicks, E., Ewing, R., Floyd, Y., Gray, K., Hall, S., Hawes, R., Hughes, J., Kosmidou, V., Menzies, A., Mould, C., Parker, A., Stevens, C., Watt, S., Hooper, S., Wilson, R., Jayatilake, H., Gusterson, B. A., Cooper, C., Shipley, J., Hargrave, D., Pritchard-Jones, K., Maitland, N., Chenevix-Trench, G., Riggins, G. J., Bigner, D. D., Palmieri, G., Cossu, A., Flanagan, A., Nicholson, A., Ho, J. W., Leung, S. Y., Yuen, S. T., Weber, B. L., Seigler, H. F., Darrow, T. L., Paterson, H., Marais, R., Marshall, C. J., Wooster, R., Stratton, M. R., and Futreal, P. A. (2002). Mutations of the BRAF gene in human cancer. Nature 417,949-954.
14. De Roock, W., Jonker, D. J., Di Nicolantonio, F., Sartore-Bianchi, A., Tu, D., Siena, S., Lamba, S., Arena, S., Frattini, M., Piessevaux, H., Van Cutsem, E., O'Callaghan, C. J., Khambata-Ford, S., Zalcberg, J. R., Simes, J., Karapetis, C. S., Bardelli, A., and Tejpar, S. (2010). Association of KRAS p.G13D mutation with outcome in patients with chemotherapy-refractory metastatic colorectal cancer treated with cetuximab. JAMA 304, 1812-1820.
15. Dummer, R., Robert, C., Chapman, P. B., Sosman, J. A., Middleton, M., Bastholt, L., Kemsley, K., Cantarini, M. V., Morris, C. and Kirkwood, J. M. (2008). AZD6244 (ARRY-142886) vs temozolomide (TMZ) in patients (pts) with advanced melanoma: an open-label, randomized, multicenter, phase II study. J. Clin. Oncol 26, 9033.
16. Fedorenko, I. V., Paraiso, K. H., and Smalley, K. S. (2011). Acquired and intrinsic BRAF inhibitor resistance in BRAF V600E mutant melanoma. Biochem. Pharmacol. 82,201-209.
17. Fornaro, L., Lucchesi, M., Caparello, C., Vasile, E., Caponi, S., Ginocchi, L., Masi, G., Falcone, A. (2011). and Medscape. Anti-HER agents in gastric cancer: from bench to bedside. Nat. Rev. Gastroenterol. Hepatol. 8, 369-383.
18. Gianni, L., Dafni, U., Gelber, R. D., Azambuja, E., Muehlbauer, S., Goldhirsch, A., Untch, M., Smith, I., Baselga, J., Jackisch, C., Cameron, D., Mano, M., Pedrini, J. L., Veronesi, A., Mendiola, C., Pluzanska, A., Semi-glazov, V., Vrdoljak, E., Eckart, M. J., Shen, Z., Skiadopoulos, G., Procter, M., Pritchard, K. I., Piccart-Gebhart, M. J., Bell, R. and Herceptin Adjuvant (HERA) Trial Study Team. (2011) Treatment with trastuzumab for 1 year after adjuvant chemotherapy in patients with HER2-positive early breast cancer: a 4-year follow-up of a randomised controlled trial. Lancet Oncol. 12,236-244.
19. Gu, L., Lau, S. K., Loera, S., Somlo, G., and Kane, S. E. (2009). Protein kinase A activation confers resistance to trastuzumab in human breast cancer cell lines. Clin. Cancer Res. 15, 7196-7206.
20. Hara, T., Miyazaki, J., Araki, H., Yamaoka, M., Kanzaki, N., Kusaka, M., and Miyamoto, M. (2003). Novel mutations of androgen receptor: a possible mechanism of bicalutamide withdrawal syndrome. Cancer Res. 63, 149-153.
21. Hilton, J. F., Amir, E., Hopkins, S., Nabavi, M., Diprimio, G., Sheikh, A., Done, S. J., Gianfelice, D., Kanji, F., Dent, S., Barth, D., Bouganim, N., Al-Najjar, A., and Clemons, M. (2010). Acquisition of metastatic tissue from patients with bone metastases from breast cancer. Breast Cancer Res. Treat. 29, 761-765.
22. Hochhaus, A., Kantarjian, H. M., Bac-carani, M., Lipton, J. H., Apperley, J. F., Druker, B. J., Facon, T., Goldberg, S. L., Cervantes, F., Niederwieser, D., Silver, R. T., Stone, R. M., Hughes, T. P., Muller, M. C., Ezzeddine, R., Countouriotis, A. M., and Shah, N. P. (2007). Dasatinib induces notable hematologic and cytoge-netic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy. Blood 109,2303-2309.
23. Infante, J. R., Falchook, G. S., Lawrence, D. P., Weber, J. S., Kefford, R. F., Bendell, J. C., Kurzrock, R., Shapiro, G., Kudchadkar, R. R., Long, G. V., Burris, H. A., Kim, K. B., Clements, A., Peng, S., Yi, B., Allred, A. J., Ouellet, D., Patel, K., Lebowitz, P. F., and Flaherty, K. T. (2011). Phase I/II study to assess safety, pharmacokinetics, and efficacy of the oral MEK 1/2 inhibitor GSK1120212 (GSK212) dosed in combination with the oral BRAF inhibitor GSK2118436 (GSK436). J. Clin. Oncol. 29(Suppl.), CRA8503.
24. Jackisch, C. (2006). HER-2-positive metastatic breast cancer: optimizing trastuzumab-based therapy. Oncologist 11(Suppl. 1), 34-41.
25. Jarry, J., Brunet, J. S., Laframboise, R., Drouin, R., Latreille, J., Richard, C., Gekas, J., Maranda, B., Monczak, Y., Wong, N., Pouchet, C., Zaor, S., Kasprzak, L., Palma, L., Wu, M. K., Tischkowitz, M., Foulkes, W. D., and Chong, G. (2011). A survey of APC mutations in Quebec. Fam. Cancer. PMID: 21779980. [Epub ahead of print].
26. Jirawatnotai, S., Hu, Y., Michowski, W., Elias, J. E., Becks, L., Bienvenu, E, Zagozdzon, A., Goswami, T., Wang, Y. E., Clark, A. B., Kunkel, T. A., van Harn, T., Xia, B., Correll, M., Quackenbush, J., Livingston, D. M., Gygi, S. P., and Sicinski, P. (2011). A function for cyclin D1 in DNA repair uncovered by protein interactome analyses in human cancers. Nature 474, 230-234.
27. Johannessen, C. M., Boehm, J. S., Kim, S. Y., Thomas, S. R., Wardwell, L., Johnson, L. A., Emery, C. M., Stran-sky, N., Cogdill, A. P., Barretina, J., Caponigro, G., Hieronymus, H., Murray, R. R., Salehi-Ashtiani, K., Hill, D. E., Vidal, M., Zhao, J. J., Yang, X., Alkan, O., Kim, S., Harris, J. L., Wilson, C. J., Myer, V. E., Finan, P. M., Root, D. E., Roberts, T. M., Golub, T., Flaherty, K. T., Dummer, R., Weber, B. L., Sellers, W R., Schlegel, R., Wargo, J. A., Hahn, W. C., and Garraway, L. A. (2010). COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 468, 968-972.
28. Kataoka, Y., Mukohara, T., Shimada, H., Saijo, N., Hirai, M., and Minami, H. (2010). Association between gain-of-function mutations in PIK3CA and resistance to HER2-targeted agents in HER2-amplified breast cancer cell lines. Ann. Oncol. 21, 255-262.
29. Kefford, R., Arkenau, H., Brown, M. P., Millward, M., Infante, J. R., Long, G. V., Ouellet, D., Curtis, M., Lebowitz, P. F., and Falchook, G. S. (2010). Phase I/II study of GSK2118436, a selective inhibitor of oncogenic mutant BRAF kinase, in patients with metastatic melanoma and other solid tumors.J. Clin. Oncol. 28,8503.
30. Khambata-Ford, S., Garrett, C. R., Meropol, N. J., Basik, M., Harbison, C T., Wu, S., Wong, T. W., Huang, X., Takimoto, C. H., Godwin, A. K.,Tan, B. R., Krishnamurthi, S. S., Burris, H. A. III, Poplin, E. A., Hidalgo, M., Baselga, J., Clark, E. A., and Mauro, D J. (2007). Expression of epireg-ulin and amphiregulin and K-ras mutation status predict disease con trol in metastatic colorectal cancer patients treated with cetuximab. J. Clin. Oncol. 25, 3230-3237.
31. Krishnan, A. V., Zhao, X. Y., Swami, S., Brive, L., Peehl, D. M., Ely, K. R., and Feldman, D. (2002). A glucocorticoid-responsive mutant androgen receptor exhibits unique ligand specificity: therapeutic implications for androgen-independent prostate cancer. Endocrinology 143, 1889-1900.
32. Lázár, V., Ecsedi, S., Szöllosi, A. G., Tóth, R., Vízkeleti, L., Rákosy, Z., Bégány, A., Adány, R., and Balázs, M. (2009). Characterization of candidate gene copy number alterations in the 11q13 region along with BRAF and NRAS mutations in human melanoma. Mod. Pathol. 22, 1367-1378.
33. Little, A. S., Balmanno, K., Sale, M. J., Newman, S., Dry, J. R., Hampson, M., Edwards, P. A., Smith, P. D., and Cook, S. J. (2011). A correction to the research article titled: "amplification of the driving oncogene, KRAS or BRAF, underpins acquired resistance to MEK1/2 inhibitors in colorectal cancer cells" by A. S. Little, K. Balmanno, M. J. Sale, S. Newman, J. R. Dry, M. Hampson, P. A. W. Edwards, P. D. Smith, S. J. Cook. Sci. Signal. 4, er2.
34. Loignon, M., Miao, W., Hu, L., Bier, A., Batist, Z., and Batist, G. (2009). Cul3 overexpression depletes Nrf2 in breast cancer and is associated with sensitivity to carcinogens, to oxida-tive stress, and to chemotherapy. Mol Cancer Ther. 8, 2432-2440.
35. Lynch, T. J., Bell, D. W., Sordella, R., Gurubhagavatula, S., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Haserlat, S. M., Supko, J. G., Haluska, F. G., Louis, D. N., Christiani, D. C., Settleman, J., and Haber, D. A. (2004). Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N. Engl. J. Med. 350,2129-2139.
36. Mackay, A., Weigelt, B., Grigoriadis, A., Kreike, B., Natrajan, R., A'Hern, R., Tan, D. S., Dowsett, M., Ashworth, A., and Reis-Filho, J. S. (2011). Microarray-based class discovery for molecular classification of breast cancer: analysis of interobserver agreement. J. Natl. Cancer Inst. 103, 662-673.
37. Miyamoto, H., Rahman, M. M., and Chang, C. S. (2004). Molecular basis for the antiandrogen withdrawal syndrome. J. Cell. Biochem. 91, 3-12.
38. Montagut, C., Sharma, S. V., Shioda, T., McDermott, U., Ulman, M., Ulkus, L. E., Dias-Santagata, D., Stubbs, H., Lee, D. Y., Singh, A., Drew, L., Haber, D. A., and Settleman, J. (2008). Elevated CRAF as apotential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 68, 4853-4861.
39. Nahta, R., and O'Regan, R. M. (2010). Evolving strategies for overcoming resistance to HER2-directed therapy: targeting the PI3K/Akt/mTOR pathway. Clin. Breast Cancer 10(Suppl. 3), S72-S78. [Review].
40. Nazarian, R., Shi, H., Wang, Q., Kong, X., Koya, R. C., Lee, H., Chen, Z., Lee, M. K., Attar, N., Sazegar, H., Chodon, T., Nelson, S. F., McArthur, G., Sosman, J. A., Ribas, A., and Lo, R. S. (2010) Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 468, 973-977.
41. Paez, J. G., Jänne, P. A., Lee, J. C., Tracy, S., Greulich, H., Gabriel, S., Herman, P., Kaye, E J., Lindeman, N., Boggon, T. J., Naoki, K., Sasaki, H., Fujii, Y., Eck, M. J., Sellers, W. R., Johnson, B. E., and Meyer-son, M. (2004). EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 304, 1497-1500.
42. Petrylak, D. P., Tangen, C. M., Hus-sain, M. H., Lara, P. N. Jr., Jones, J. A., Taplin, M. E., Burch, P. A., Berry, D., Moinpour, C., Kohli, M., Benson, M. C., Small, E. J., Raghavan, D., and Crawford, E. D. (2004). Docetaxel and estramustine compared with mitoxantrone and prednisone for advanced refractory prostate cancer. N. Engl. J. Med. 351, 1513-1520.
43. Press, M. F., Sauter, G., Bernstein, L., Vil-lalobos, I. E., Mirlacher, M., Zhou, J. Y., Wardeh, R., Li, Y. T., Guzman, R., Ma, Y., Sullivan-Halley, J., Santiago, A., Park, J. M., Riva, A., and Sla-mon, D. J. (2005). Diagnostic evaluation of HER-2 as a molecular target: an assessment of accuracy and reproducibility of laboratory testing in large, prospective, randomized clinical trials. Clin. Cancer Res. 11, 6598-6607.
44. Ren, D., Villeneuve, N. F., Jiang, T., Wu, T., Lau, A., Toppin, H., and Zhang, D. D. (2011). Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Proc. Natl Acad. Sci. U.S.A. 108, 1433-1438.
45. Ryan, C. J., and Tindall, D. J. (2011). Androgen receptor rediscovered: the new biology and targeting the androgen receptor therapeutically. J. Clin. Oncol. 29, 3651-3658.
46. Sakai, W., Swisher, E. M., Karlan, B. Y., Agarwal, M. K., Higgins, J., Friedman, C., Villegas, E., Jacque-mont, C., Farrugia, D. J., Couch, F. J., Urban, N., and Taniguchi, T. (2008). Secondary mutations as a mechanism of cisplatin resistance in BRCA2-mutated cancers. Nature 451, 1116-1120.
47. Sartore-Bianchi, A., Di Nicolantonio, E, Nichelatti, M., Molinari, F., De Dosso, S., Saletti, P., Martini, M., Cipani, T., Marrapese, G., Mazzucchelli, L., Lamba, S., Veronese, S., Frattini, M., Bardelli, A., and Siena, S. (2009). Multi-determinants analysis of molecular alterations for predicting clinical benefit to EGFR-targeted monoclonal antibodies in colorec-tal cancer. PLoS ONE 4, e7287. doi:10.1371/journal.pone.0007287
48. Sasaki, T., Koivunen, J., Ogino, A., Yanagita, M., Nikiforow, S., Zheng, W., Lathan, C., Marcoux, J. P., Du, J., Okuda, K., Capelletti, M., Shima-mura, T., Ercan, D., Stumpfova, M., Xiao, Y., Weremowicz, S., Butaney, M., Heon, S., Wilner, K., Christensen, J. G., Eck, M. J., Wong, K. K., Lindeman, N., Gray, N. S., Rodig, S. J., and Janne, P. A. (2011). A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res. 71, 6051-6060.
49. Shah, N. P., Nicoll, J. M., Nagar, B., Gorre, M. E., Paquette, R. L., Kuriyan, J., and Sawyers, C. L. (2002). Multiple BCR-ABL kinase domain mutations confer poly-clonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2,117-125.
50. Sharfman, W H., Hodi, E S., Lawrence, D. P., Flaherty, K. T., Amaravadi, R. K., Kim, K. B., Dummer, R., Gobbi, S., Puzanov, I., Sosman, J. A., Dohoney, K., Lam, L. P., Kakar, S., Tang, Z., Krieter, O., and Atkins, M. B. (2011) Results from the first-inhuman (FIH) phase I study of the oral RAF inhibitor RAF265 administered daily to patients with advanced cutaneous melanoma. J. Clin. Oncol. 29,8508.
51. Singh, A., Boldin-Adamsky, S., Thim-mulappa, R. K., Rath, S. K., Ashush, H., Coulter, J., Blackford, A., Goodman, S. N., Bunz, F., Watson, W. H., Gabrielson, E., Feinstein, E., and Biswal, S. (2008). RNAi-mediated silencing of Nrf-2-related factor 2 gene expression in non-small cell lung cancer inhibits tumor growth and increases efficacy of chemotherapy. Cancer Res. 68, 7975-7984.
52. Singh, A., Misra, V., Thimmulappa, R. K., Lee, H., Ames, S., Hoque, M. O., Herman, J. G., Baylin, S. B., Sidransky, D., Gabrielson, E., Brock, M. V., and Biswal, S. (2006). Dysfunctional KEAP1-NRF2 interaction in non-small-cell lung cancer. PLoS Med. 3, 1865-1876. doi:10.1371/journal.pmed.0030420
53. Smalley, K. S., Lioni, M., Dalla Palma, M., Xiao, M., Desai, B., Egyhazi, S., Hansson, J., Wu, H., King, A. J., Van Belle, P., Elder, D. E., Flaherty, K. T., Herlyn, M., and Nathanson, K. L. (2008). Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas. Mol. Cancer Ther. 7, 2876-2883.
54. Steketee, K., Timmerman, L., Ziel-van der Made, A. C. J., Doesburg, P., Brinkmann, A. O., and Trapman, J. (2002). Broadened ligand responsiveness of androgen receptor mutants obtained by random amino acid substitution of H874 and mutation hot spot T877 in prostate cancer. Int. J. Cancer 100, 309-317.
55. Tannock, I. F., de Wit, R., Berry, W R., Horti, J., Pluzanska, A., Chi, K. N., Oudard, S., Théodore, C., James, N. D., Turesson, I., Rosenthal, M. A., Eisenberger, M. A. and TAX 327 Investigators. (2004). Docetaxel plus prednisone or mitoxantroneplus prednisone for advanced prostate cancer. N Engl. J. Med. 351, 1502-1512.
56. Taplin, M. E. (2008). Androgen receptor: role and novel therapeutic prospects in prostate cancer. Expert Rev. Anticancer Ther. 8, 1495-1508.
57. Taplin, M. E., and Ho, S. M. (2001). The endocrinology of prostate cancer. J. Clin. Endocrinol. Metab. 86, 3467-3477.
58. Taplin, M. E., Rajeshkumar, B., Halabi, S., Werner, C. P., Woda, B. A., Picus, J., Stadler, W., Hayes, D. F., Kantoff, P. W., Vogelzang, N. J., Small, E. J., and Cancer and Leukemia Group B Study 9663. (2003). Androgen receptor mutations in androgen-in dependent prostate cancer: Cancer and Leukemia Group B Study 9663. J. Clin. Oncol. 21,2673-2678.
59. Urushibara, M., Ishioka, J., Hyochi, N., Kihara, K., Hara, S., Singh, P., Isaacs,J.T.,andKageyama,Y (2007). Effects of steroidal and non-steroidal antiandrogens on wild-type and mutant androgen receptors. Prostate 67, 799-807.
60. Villanueva, J., Vultur, A., Lee, J. T., Soma-sundaram, R., Fukunaga-Kalabis, M., Cipolla, A. K., Wubbenhorst, B., Xu, X., Gimotty, P. A., Kee, D., Santiago-Walker, A. E., Letrero, R., D'Andrea, K., Pushparajan, A., Hay-den, J. E., Brown, K. D., Laque-rre, S., McArthur, G. A., Sosman, J. A., Nathanson, K. L., and Herlyn, M. (2010). Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K. Cancer Cell 18, 683-695.
61. Wagle, N., Caroline, E., Berger, M. F., Davis, M. J., Sawyer, A., Pochanard, P., Kehoe, S. M., Johannessen, C. M., MacConaill, L. E., Hahn, W. C., Meyerson, M., and Garraway, L. A. (2011). Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J. Clin. Oncol. 29, 3085-3096.
62. Wan, P. T., Garnett, M. J., Roe, S. M., Lee, S., Niculescu-Duvaz, D., Good, V M., Jones, C. M., Marshall, C. J., Springer, C. J., Barford, D., Marais, R., and Cancer Genome Project. (2004). Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell 116,855-867.
63. Wu, J. Y., Wu, S. G., Yang, C. H., Gow, C. H., Chang, Y L, Yu, C. J., Shih, J. Y., and Yang, P. C. (2008). Lung cancer with epidermal growth factor receptor exon 20 mutations is associated with poor gefitinib treatment response. Clin. Cancer Res. 14, 4877-4882.
64. Zhang, S., Huang, W. C., Li, P., Guo, H., Poh, S. B., Brady, S. W., Xiong, Y., Tseng, L. M., Li, S. H., Ding, Z., Sahin, A. A., Esteva, F. J., Hortobagyi, G. N., and Yu, D. (2011) Combating trastuzumab resistance by targeting SRC, a common node downstream of multiple resistance pathways. Nat. Med. 17,461-469.
65. Zhou, J., Geng, G., Shi, Q., Sauriol, E, and Wu, J. H. (2009). Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance. J. Med. Chem. 52, 5546-5550.