Drug resistance to targeted therapies: Déjà vu all over again

Molecular Oncology

Volumn 8, Issue 6, 2014, Pages 1067-1083

  Groenendijk, Floris H ^a   Bernards, René ^a  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

Author keywords

Anticancer therapy; Drug combinations; Drug resistance; Endocrine therapy; Pathway reactivation; Targeted therapy

Indexed keywords

AFATINIB; CETUXIMAB; CRIZOTINIB; DABRAFENIB; DOCETAXEL; ERLOTINIB; ESTROGEN RECEPTOR ALPHA; EVEROLIMUS; GEFITINIB; IMATINIB; LAPATINIB; LETROZOLE; PALBOCICLIB; PERTUZUMAB; TAMOXIFEN; TRAMETINIB; TRASTUZUMAB; VEMURAFENIB; ANTINEOPLASTIC AGENT;

BREAST CANCER; CANCER COMBINATION CHEMOTHERAPY; CANCER HORMONE THERAPY; CANCER RESISTANCE; DRUG EFFICACY; GENE MUTATION; HUMAN; MONOTHERAPY; NONHUMAN; OUTCOME ASSESSMENT; OVERALL SURVIVAL; PATIENT MONITORING; PROGRESSION FREE SURVIVAL; REVIEW; SIGNAL TRANSDUCTION; TREATMENT INDICATION; ANIMAL; DRUG EFFECTS; DRUG RESISTANCE; METABOLISM; MOLECULARLY TARGETED THERAPY; NEOPLASMS;

ANIMALS; ANTINEOPLASTIC AGENTS; DRUG RESISTANCE, NEOPLASM; HUMANS; MOLECULAR TARGETED THERAPY; NEOPLASMS; SIGNAL TRANSDUCTION;

EID: 84913536390     PISSN: 15747891     EISSN: 18780261     Source Type: Journal    
DOI: 10.1016/j.molonc.2014.05.004     Document Type: Review

References (129)

1. Albertson D.G. ESR1 amplification in breast cancer: controversy resolved?. J.Pathol. 2012, 227:1-3.
2. Amado R.G., Wolf M., Peeters M., Van Cutsem E., Siena S., Freeman D.J., Juan T., Sikorski R., Suggs S., Radinsky R., Patterson S.D., Chang D.D. Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer. J.Clin. Oncol. 2008, 26:1626-1634.
3. Arpino G., Green S.J., Allred D.C., Lew D., Martino S., Osborne C.K., Elledge R.M. HER-2 amplification, HER-1 expression, and tamoxifen response in estrogen receptor-positive metastatic breast cancer: a southwest oncology group study. Clin. Cancer Res. 2004, 10:5670-5676.
4. Awad M.M., Katayama R., McTigue M., Liu W., Deng Y.L., Brooun A., Friboulet L., Huang D., Falk M.D., Timofeevski S., Wilner K.D., Lockerman E.L., Khan T.M., Mahmood S., Gainor J.F., Digumarthy S.R., Stone J.R., Mino-Kenudson M., Christensen J.G., Iafrate A.J., Engelman J.A., Shaw A.T. Acquired resistance to crizotinib from a mutation in CD74-ROS1. N.Engl. J. Med. 2013, 368:2395-2401.
5. Bachelot T., Bourgier C., Cropet C., Ray-Coquard I., Ferrero J.M., Freyer G., Abadie-Lacourtoisie S., Eymard J.C., Debled M., Spaeth D., Legouffe E., Allouache D., El Kouri C., Pujade-Lauraine E. Randomized phase II trial of everolimus in combination with tamoxifen in patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative metastatic breast cancer with prior exposure to aromatase inhibitors: a GINECO study. J.Clin. Oncol. 2012, 30:2718-2724.
6. Bardelli A., Corso S., Bertotti A., Hobor S., Valtorta E., Siravegna G., Sartore-Bianchi A., Scala E., Cassingena A., Zecchin D., Apicella M., Migliardi G., Galimi F., Lauricella C., Zanon C., Perera T., Veronese S., Corti G., Amatu A., Gambacorta M., Diaz L.A., Sausen M., Velculescu V.E., Comoglio P., Trusolino L., Di Nicolantonio F., Giordano S., Siena S. Amplification of the MET receptor drives resistance to anti-EGFR therapies in colorectal cancer. Cancer Discov. 2013, 3:658-673.
7. Baselga J., Bradbury I., Eidtmann H., Di Cosimo S., de Azambuja E., Aura C., Gomez H., Dinh P., Fauria K., Van Dooren V., Aktan G., Goldhirsch A., Chang T.W., Horvath Z., Coccia-Portugal M., Domont J., Tseng L.M., Kunz G., Sohn J.H., Semiglazov V., Lerzo G., Palacova M., Probachai V., Pusztai L., Untch M., Gelber R.D., Piccart-Gebhart M., Neo A.S.T. Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): a randomised, open-label, multicentre, phase 3 trial. Lancet 2012, 379:633-640.
8. Baselga J., Campone M., Piccart M., Burris H.A., Rugo H.S., Sahmoud T., Noguchi S., Gnant M., Pritchard K.I., Lebrun F., Beck J.T., Ito Y., Yardley D., Deleu I., Perez A., Bachelot T., Vittori L., Xu Z., Mukhopadhyay P., Lebwohl D., Hortobagyi G.N. Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer. N.Engl. J. Med. 2012, 366:520-529.
9. Baselga J., Cortes J., Kim S.B., Im S.A., Hegg R., Im Y.H., Roman L., Pedrini J.L., Pienkowski T., Knott A., Clark E., Benyunes M.C., Ross G., Swain S.M. Pertuzumab plus trastuzumab plus docetaxel for metastatic breast cancer. N.Engl. J. Med. 2012, 366:109-119.
10. Beelen K., Zwart W., Linn S.C. Can predictive biomarkers in breast cancer guide adjuvant endocrine therapy?. Nat. Rev. Clin. Oncol. 2012, 9:529-541.
11. Berns K., Horlings H.M., Hennessy B.T., Madiredjo M., Hijmans E.M., Beelen K., Linn S.C., Gonzalez-Angulo A.M., Stemke-Hale K., Hauptmann M., Beijersbergen R.L., Mills G.B., van de Vijver M.J., Bernards R. A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer. Cancer Cell 2007, 12:395-402.
12. Berns K., Bernards R. Understanding resistance to targeted cancer drugs through loss of function genetic screens. Drug Resist Updat. 2013, 15:268-275.
13. Berra Y. The Yogi Book: "I Really Didn't Say Everything I Said!" 1998, Workman Publishing Company, Inc.
14. Bollag G., Hirth P., Tsai J., Zhang J., Ibrahim P.N., Cho H., Spevak W., Zhang C., Zhang Y., Habets G., Burton E.A., Wong B., Tsang G., West B.L., Powell B., Shellooe R., Marimuthu A., Nguyen H., Zhang K.Y., Artis D.R., Schlessinger J., Su F., Higgins B., Iyer R., D'Andrea K., Koehler A., Stumm M., Lin P.S., Lee R.J., Grippo J., Puzanov I., Kim K.B., Ribas A., McArthur G.A., Sosman J.A., Chapman P.B., Flaherty K.T., Xu X., Nathanson K.L., Nolop K. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 2010, 467:596-599.
15. Bose R., Kavuri S.M., Searleman A.C., Shen W., Shen D., Koboldt D.C., Monsey J., Goel N., Aronson A.B., Li S., Ma C.X., Ding L., Mardis E.R., Ellis M.J. Activating HER2 mutations in HER2 gene amplification negative breast cancer. Cancer Discov. 2013, 3:224-237.
16. Bozic I., Reiter J.G., Allen B., Antal T., Chatterjee K., Shah P., Moon Y.S., Yaqubie A., Kelly N., Le D.T., Lipson E.J., Chapman P.B., Diaz L.A., Vogelstein B., Nowak M.A. Evolutionary dynamics of cancer in response to targeted combination therapy. Elife 2013, 2:e00747.
17. Brockman R.W. Mechanisms of resistance to anticancer agents. Adv. Cancer Res. 1963, 7:129-234.
18. Brummelkamp T.R., Bernards R., Agami R. A system for stable expression of short interfering RNAs in mammalian cells. Science 2002, 296:550-553.
19. Brunen D., Willems S.M., Kellner U., Midgley R., Simon I., Bernards R. TGF-beta: an emerging player in drug resistance. Cell Cycle 2013, 12:2960-2968.
20. Byers L.A., Diao L., Wang J., Saintigny P., Girard L., Peyton M., Shen L., Fan Y., Giri U., Tumula P.K., Nilsson M.B., Gudikote J., Tran H., Cardnell R.J., Bearss D.J., Warner S.L., Foulks J.M., Kanner S.B., Gandhi V., Krett N., Rosen S.T., Kim E.S., Herbst R.S., Blumenschein G.R., Lee J.J., Lippman S.M., Ang K.K., Mills G.B., Hong W.K., Weinstein J.N., Wistuba, Coombes K.R., Minna J.D., Heymach J.V. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance. Clin. Cancer Res. 2013, 19:279-290.
21. Cancer Genome Atlas Network Comprehensive molecular portraits of human breast tumours. Nature 2012, 490:61-70.
22. Chandarlapaty S., Sawai A., Scaltriti M., Rodrik-Outmezguine V., Grbovic-Huezo O., Serra V., Majumder P.K., Baselga J., Rosen N. AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity. Cancer Cell 2011, 19:58-71.
23. 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., Schadendorf D., Ribas A., O'Day S.J., Sosman J.A., Kirkwood J.M., Eggermont A.M., Dreno B., Nolop K., Li J., Nelson B., Hou J., Lee R.J., Flaherty K.T., McArthur G.A. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N.Engl. J. Med. 2011, 364:2507-2516.
24. 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., Mano H. EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors. N.Engl. J. Med. 2010, 363:1734-1739.
25. Corcoran R.B., Dias-Santagata D., Bergethon K., Iafrate A.J., Settleman J., Engelman J.A. BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutation. Sci. Signal. 2010, 3:ra84.
26. Corcoran R.B., Ebi H., Turke A.B., Coffee E.M., Nishino M., Cogdill A.P., Brown R.D., Della Pelle P., Dias-Santagata D., Hung K.E., Flaherty K.T., Piris A., Wargo J.A., Settleman J., Mino-Kenudson M., Engelman J.A. EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib. Cancer Discov. 2012, 2:227-235.
27. Crowley E., Di Nicolantonio F., Loupakis F., Bardelli A. Liquid biopsy: monitoring cancer-genetics in the blood. Nat. Rev. Clin. Oncol. 2013, 10:472-484.
28. Das Thakur M., Salangsang F., Landman A.S., Sellers W.R., Pryer N.K., Levesque M.P., Dummer R., McMahon M., Stuart D.D. Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance. Nature 2013, 494:251-255.
29. Davies C., Godwin J., Gray R., Clarke M., Cutter D., Darby S., McGale P., Pan H.C., Taylor C., Wang Y.C., Dowsett M., Ingle J., Peto R. Relevance of breast cancer hormone receptors and other factors to the efficacy of adjuvant tamoxifen: patient-level meta-analysis of randomised trials. Lancet 2011, 378:771-784.
30. Davies K.D., Le A.T., Theodoro M.F., Skokan M.C., Aisner D.L., Berge E.M., Terracciano L.M., Cappuzzo F., Incarbone M., Roncalli M., Alloisio M., Santoro A., Camidge D.R., Varella-Garcia M., Doebele R.C. Identifying and targeting ROS1 gene fusions in non-small cell lung cancer. Clin. Cancer Res. 2012, 18:4570-4579.
31. De Laurentiis M., Arpino G., Massarelli E., Ruggiero A., Carlomagno C., Ciardiello F., Tortora G., D'Agostino D., Caputo F., Cancello G., Montagna E., Malorni L., Zinno L., Lauria R., Bianco A.R., De Placido S. A meta-analysis on the interaction between HER-2 expression and response to endocrine treatment in advanced breast cancer. Clin. Cancer Res. 2005, 11:4741-4748.
32. Diaz L.A., Williams R.T., Wu J., Kinde I., Hecht J.R., Berlin J., Allen B., Bozic I., Reiter J.G., Nowak M.A., Kinzler K.W., Oliner K.S., Vogelstein B. The molecular evolution of acquired resistance to targeted EGFR blockade in colorectal cancers. Nature 2012, 486:537-540.
33. Duncan J.S., Whittle M.C., Nakamura K., Abell A.N., Midland A.A., Zawistowski J.S., Johnson N.L., Granger D.A., Jordan N.V., Darr D.B., Usary J., Kuan P.F., Smalley D.M., Major B., He X., Hoadley K.A., Zhou B., Sharpless N.E., Perou C.M., Kim W.Y., Gomez S.M., Chen X., Jin J., Frye S.V., Earp H.S., Graves L.M., Johnson G.L. Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer. Cell 2012, 149:307-321.
34. EBCTCG Effects of chemotherapy and hormonal therapy for early breast cancer on recurrence and 15-year survival: an overview of the randomised trials. Lancet 2005, 365:1687-1717.
35. Emery C.M., Vijayendran K.G., Zipser M.C., Sawyer A.M., Niu L., Kim J.J., Hatton C., Chopra R., Oberholzer P.A., Karpova M.B., MacConaill L.E., Zhang J., Gray N.S., Sellers W.R., Dummer R., Garraway L.A. MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc. Natl. Acad. Sci. U.S.A. 2009, 106:20411-20416.
36. Encarnacion C.A., Ciocca D.R., McGuire W.L., Clark G.M., Fuqua S.A., Osborne C.K. Measurement of steroid hormone receptors in breast cancer patients on tamoxifen. Breast Cancer Res. Treat. 1993, 26:237-246.
37. Engelman J.A., Zejnullahu K., Mitsudomi T., Song Y., Hyland C., Park J.O., Lindeman N., Gale C.M., Zhao X., Christensen J., Kosaka T., Holmes A.J., Rogers A.M., Cappuzzo F., Mok T., Lee C., Johnson B.E., Cantley L.C., Janne P.A. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007, 316:1039-1043.
38. Finn R.S., Crown J.P., Lang I., Boer K., Bondarenko I.M., Kulyk S.O., Ettl J., Patel R., Pinter T., Schmidt M., Shparyk Y., Thummala A.R., Voytko N.L., Breazna A., Kim S.T., Randolph S., Slamon D.J. Results of a randomized phase 2 study of PD 0332991, a cyclin-dependent kinase (CDK) 4/6 inhibitor, in combination with letrozole vs letrozole alone for first-line treatment of ER+/HER2- advanced breast cancer (BC). Cancer Res. 2012, 72(24 Suppl.). Abstract nr S1-S6.
39. Flaherty K.T., Infante J.R., Daud A., Gonzalez R., Kefford R.F., Sosman J., Hamid O., Schuchter L., Cebon J., Ibrahim N., Kudchadkar R., Burris H.A., Falchook G., Algazi A., Lewis K., Long G.V., Puzanov I., Lebowitz P., Singh A., Little S., Sun P., Allred A., Ouellet D., Kim K.B., Patel K., Weber J. Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N.Engl. J. Med. 2012, 367:1694-1703.
40. Fuchs B.C., Fujii T., Dorfman J.D., Goodwin J.M., Zhu A.X., Lanuti M., Tanabe K.K. Epithelial-to-mesenchymal transition and integrin-linked kinase mediate sensitivity to epidermal growth factor receptor inhibition in human hepatoma cells. Cancer Res. 2008, 68:2391-2399.
41. Girotti M.R., Pedersen M., Sanchez-Laorden B., Viros A., Turajlic S., Niculescu-Duvaz D., Zambon A., Sinclair J., Hayes A., Gore M., Lorigan P., Springer C., Larkin J., Jorgensen C., Marais R. Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma. Cancer Discov. 2013, 3:158-167.
42. Goetz M.P., Rae J.M., Suman V.J., Safgren S.L., Ames M.M., Visscher D.W., Reynolds C., Couch F.J., Lingle W.L., Flockhart D.A., Desta Z., Perez E.A., Ingle J.N. Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes. J.Clin. Oncol. 2005, 23:9312-9318.
43. Gorre M.E., Mohammed M., Ellwood K., Hsu N., Paquette R., Rao P.N., Sawyers C.L. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science 2001, 293:876-880.
44. Groenendijk F.H., Zwart W., Floore A., Akbari S., Bernards R. Estrogen receptor splice variants as a potential source of false-positive estrogen receptor status in breast cancer diagnostics. Breast Cancer Res. Treat. 2013, 140:475-484.
45. Gururaj A.E., Rayala S.K., Vadlamudi R.K., Kumar R. Novel mechanisms of resistance to endocrine therapy: genomic and nongenomic considerations. Clin. Cancer Res. 2006, 12:1001s-1007s.
46. Gutierrez M.C., Detre S., Johnston S., Mohsin S.K., Shou J., Allred D.C., Schiff R., Osborne C.K., Dowsett M. Molecular changes in tamoxifen-resistant breast cancer: relationship between estrogen receptor, HER-2, and p38 mitogen-activated protein kinase. J.Clin. Oncol. 2005, 23:2469-2476.
47. Haughian J.M., Pinto M.P., Harrell J.C., Bliesner B.S., Joensuu K.M., Dye W.W., Sartorius C.A., Tan A.C., Heikkila P., Perou C.M., Horwitz K.B. Maintenance of hormone responsiveness in luminal breast cancers by suppression of Notch. Proc. Natl. Acad. Sci. U.S.A. 2012, 109:2742-2747.
48. Hemeryck A., Belpaire F.M. Selective serotonin reuptake inhibitors and cytochrome P-450 mediated drug-drug interactions: an update. Curr. Drug Metab. 2002, 3:13-37.
49. Herynk M.H., Fuqua S.A. Estrogen receptor mutations in human disease. Endocr. Rev. 2004, 25:869-898.
50. Holm C., Kok M., Michalides R., Fles R., Koornstra R.H., Wesseling J., Hauptmann M., Neefjes J., Peterse J.L., Stal O., Landberg G., Linn S.C. Phosphorylation of the oestrogen receptor alpha at serine 305 and prediction of tamoxifen resistance in breast cancer. J.Pathol. 2009, 217:372-379.
51. Hoskins J.M., Carey L.A., McLeod H.L. CYP2D6 and tamoxifen: DNA matters in breast cancer. Nat. Rev. Cancer 2009, 9:576-586.
52. Huang S., Holzel M., Knijnenburg T., Schlicker A., Roepman P., McDermott U., Garnett M., Grernrum W., Sun C., Prahallad A., Groenendijk F.H., Mittempergher L., Nijkamp W., Neefjes J., Salazar R., Ten Dijke P., Uramoto H., Tanaka F., Beijersbergen R.L., Wessels L.F., Bernards R. MED12 controls the response to multiple cancer drugs through regulation of TGF-beta receptor signaling. Cell 2012, 151:937-950.
53. Iorns E., Turner N.C., Elliott R., Syed N., Garrone O., Gasco M., Tutt A.N., Crook T., Lord C.J., Ashworth A. Identification of CDK10 as an important determinant of resistance to endocrine therapy for breast cancer. Cancer Cell 2008, 13:91-104.
54. Jeselsohn R., Yelensky R., Buchwalter G., Frampton G., Meric-Bernstam F., Gonzalez-Angulo A.M., Ferrer-Lozano J., Perez-Fidalgo J.A., Cristofanilli M., Gomez H., Arteaga C.L., Giltnane J., Balko J.M., Cronin M.T., Jarosz M., Sun J., Hawryluk M., Lipson D., Otto G., Ross J.S., Dvir A., Soussan-Gutman L., Wolf I., Rubinek T., Gilmore L., Schnitt S., Come S.E., Pusztai L., Stephens P., Brown M., Miller V.A. Emergence of constitutively active estrogen receptor-alpha mutations in pretreated advanced estrogen receptor-positive breast cancer. Clin. Cancer Res. 2014, 20:1757-1767.
55. Johannessen C.M., Boehm J.S., Kim S.Y., Thomas S.R., Wardwell L., Johnson L.A., Emery C.M., Stransky 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., Garraway L.A. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 2010, 468:968-972.
56. Johannessen C.M., Johnson L.A., Piccioni F., Townes A., Frederick D.T., Donahue M.K., Narayan R., Flaherty K.T., Wargo J.A., Root D.E., Garraway L.A. A melanocyte lineage program confers resistance to MAP kinase pathway inhibition. Nature 2013, 504:138-142.
57. Johnston S.R., Saccani-Jotti G., Smith I.E., Salter J., Newby J., Coppen M., Ebbs S.R., Dowsett M. Changes in estrogen receptor, progesterone receptor, and pS2 expression in tamoxifen-resistant human breast cancer. Cancer Res. 1995, 55:3331-3338.
58. Karapetis C.S., Khambata-Ford S., Jonker D.J., O'Callaghan C.J., Tu D., Tebbutt N.C., Simes R.J., Chalchal H., Shapiro J.D., Robitaille S., Price T.J., Shepherd L., Au H.J., Langer C., Moore M.J., Zalcberg J.R. K-ras mutations and benefit from cetuximab in advanced colorectal cancer. N.Engl. J. Med. 2008, 359:1757-1765.
59. Katayama R., Shaw A.T., Khan T.M., Mino-Kenudson M., Solomon B.J., Halmos B., Jessop N.A., Wain J.C., Yeo A.T., Benes C., Drew L., Saeh J.C., Crosby K., Sequist L.V., Iafrate A.J., Engelman J.A. Mechanisms of acquired crizotinib resistance in ALK-rearranged lung cancers. Sci. Transl. Med. 2012, 4:120ra117.
60. Kim Y., Ko J., Cui Z., Abolhoda A., Ahn J.S., Ou S.H., Ahn M.J., Park K. The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor. Mol. Cancer Ther. 2012, 11:784-791.
61. Kobayashi S., Boggon T.J., Dayaram T., Janne P.A., Kocher O., Meyerson M., Johnson B.E., Eck M.J., Tenen D.G., Halmos B. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N.Engl. J. Med. 2005, 352:786-792.
62. Kuukasjarvi T., Kononen J., Helin H., Holli K., Isola J. Loss of estrogen receptor in recurrent breast cancer is associated with poor response to endocrine therapy. J.Clin. Oncol. 1996, 14:2584-2589.
63. Lemmon M.A., Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell 2010, 141:1117-1134.
64. Li S., Shen D., Shao J., Crowder R., Liu W., Prat A., He X., Liu S., Hoog J., Lu C., Ding L., Griffith O.L., Miller C., Larson D., Fulton R.S., Harrison M., Mooney T., McMichael J.F., Luo J., Tao Y., Goncalves R., Schlosberg C., Hiken J.F., Saied L., Sanchez C., Giuntoli T., Bumb C., Cooper C., Kitchens R.T., Lin A., Phommaly C., Davies S.R., Zhang J., Kavuri M.S., McEachern D., Dong Y.Y., Ma C., Pluard T., Naughton M., Bose R., Suresh R., McDowell R., Michel L., Aft R., Gillanders W., DeSchryver K., Wilson R.K., Wang S., Mills G.B., Gonzalez-Angulo A., Edwards J.R., Maher C., Perou C.M., Mardis E.R., Ellis M.J. Endocrine-therapy-resistant ESR1 variants revealed by genomic characterization of breast-cancer-derived xenografts. Cell Rep. 2013, 4:1116-1130.
65. Little A.S., Balmanno K., Sale M.J., Newman S., Dry J.R., Hampson M., Edwards P.A., Smith P.D., Cook S.J. Amplification of the driving oncogene, KRAS or BRAF, underpins acquired resistance to MEK1/2 inhibitors in colorectal cancer cells. Sci. Signal. 2011, 4:ra17.
66. Long G.V., Menzies A.M., Nagrial A.M., Haydu L.E., Hamilton A.L., Mann G.J., Hughes T.M., Thompson J.F., Scolyer R.A., Kefford R.F. Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma. J.Clin. Oncol. 2011, 29:1239-1246.
67. Maemondo M., Inoue A., Kobayashi K., Sugawara S., Oizumi S., Isobe H., Gemma A., Harada M., Yoshizawa H., Kinoshita I., Fujita Y., Okinaga S., Hirano H., Yoshimori K., Harada T., Ogura T., Ando M., Miyazawa H., Tanaka T., Saijo Y., Hagiwara K., Morita S., Nukiwa T. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N.Engl. J. Med. 2010, 362:2380-2388. North-East Japan Study, G.
68. Magnani L., Stoeck A., Zhang X., Lanczky A., Mirabella A.C., Wang T.L., Gyorffy B., Lupien M. Genome-wide reprogramming of the chromatin landscape underlies endocrine therapy resistance in breast cancer. Proc. Natl. Acad. Sci. U.S.A. 2013, 110:E1490-E1499.
69. Majewski, I.J., Nuciforo, P., Mittempergher, L., Bosma, A.J., Eidtmann, H., Holmes, E., Sotiriou, C., Fumagalli, D., Jimenez, J., Aura, C., Prudkin, L., Delgado, M.C.D., de la Pena, L., Loi, S., GSK TBDef, de Azambuja, E., Harbeck, N., Piccart-Gebhart, M., Bernards, R., Baselga, J., 2014. PIK3CA mutations are associated with resistance to neoadjuvant HER2-targeted therapies in breast cancer, submitted for publication.
70. McGlynn L.M., Kirkegaard T., Edwards J., Tovey S., Cameron D., Twelves C., Bartlett J.M., Cooke T.G. Ras/Raf-1/MAPK pathway mediates response to tamoxifen but not chemotherapy in breast cancer patients. Clin. Cancer Res. 2009, 15:1487-1495.
71. Michalides R., Griekspoor A., Balkenende A., Verwoerd D., Janssen L., Jalink K., Floore A., Velds A., van't Veer L., Neefjes J. Tamoxifen resistance by a conformational arrest of the estrogen receptor alpha after PKA activation in breast cancer. Cancer Cell 2004, 5:597-605.
72. Michor F., Hughes T.P., Iwasa Y., Branford S., Shah N.P., Sawyers C.L., Nowak M.A. Dynamics of chronic myeloid leukaemia. Nature 2005, 435:1267-1270.
73. Miller T.W., Balko J.M., Arteaga C.L. Phosphatidylinositol 3-kinase and antiestrogen resistance in breast cancer. J.Clin. Oncol. 2011, 29:4452-4461.
74. Miller T.W., Balko J.M., Ghazoui Z., Dunbier A., Anderson H., Dowsett M., Gonzalez-Angulo A.M., Mills G.B., Miller W.R., Wu H., Shyr Y., Arteaga C.L. A gene expression signature from human breast cancer cells with acquired hormone independence identifies MYC as a mediator of antiestrogen resistance. Clin. Cancer Res. 2011, 17:2024-2034.
75. Misale S., Yaeger R., Hobor S., Scala E., Janakiraman M., Liska D., Valtorta E., Schiavo R., Buscarino M., Siravegna G., Bencardino K., Cercek A., Chen C.T., Veronese S., Zanon C., Sartore-Bianchi A., Gambacorta M., Gallicchio M., Vakiani E., Boscaro V., Medico E., Weiser M., Siena S., Di Nicolantonio F., Solit D., Bardelli A. Emergence of KRAS mutations and acquired resistance to anti-EGFR therapy in colorectal cancer. Nature 2012, 486:532-536.
76. Montagut C., Dalmases A., Bellosillo B., Crespo M., Pairet S., Iglesias M., Salido M., Gallen M., Marsters S., Tsai S.P., Minoche A., Seshagiri S., Serrano S., Himmelbauer H., Bellmunt J., Rovira A., Settleman J., Bosch F., Albanell J. Identification of a mutation in the extracellular domain of the epidermal growth factor receptor conferring cetuximab resistance in colorectal cancer. Nat. Med. 2012, 18:221-223.
77. Montero-Conde C., Ruiz-Llorente S., Dominguez J.M., Knauf J.A., Viale A., Sherman E.J., Ryder M., Ghossein R.A., Rosen N., Fagin J.A. Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas. Cancer Discov. 2013, 3:520-533.
78. Musgrove E.A., Sutherland R.L. Biological determinants of endocrine resistance in breast cancer. Nat. Rev. Cancer 2009, 9:631-643.
79. Nagata Y., Lan K.H., Zhou X., Tan M., Esteva F.J., Sahin A.A., Klos K.S., Li P., Monia B.P., Nguyen N.T., Hortobagyi G.N., Hung M.C., Yu D. PTEN activation contributes to tumor inhibition by trastuzumab, and loss of PTEN predicts trastuzumab resistance in patients. Cancer Cell 2004, 6:117-127.
80. Nathanson D.A., Gini B., Mottahedeh J., Visnyei K., Koga T., Gomez G., Eskin A., Hwang K., Wang J., Masui K., Paucar A., Yang H., Ohashi M., Zhu S., Wykosky J., Reed R., Nelson S.F., Cloughesy T.F., James C.D., Rao P.N., Kornblum H.I., Heath J.R., Cavenee W.K., Furnari F.B., Mischel P.S. Targeted therapy resistance mediated by dynamic regulation of extrachromosomal mutant EGFR DNA. Science 2014, 343:72-76.
81. 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., Lo R.S. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 2010, 468:973-977.
82. O'Hare T., Shakespeare W.C., Zhu X., Eide C.A., Rivera V.M., Wang F., Adrian L.T., Zhou T., Huang W.S., Xu Q., Metcalf C.A., Tyner J.W., Loriaux M.M., Corbin A.S., Wardwell S., Ning Y., Keats J.A., Wang Y., Sundaramoorthi R., Thomas M., Zhou D., Snodgrass J., Commodore L., Sawyer T.K., Dalgarno D.C., Deininger M.W., Druker B.J., Clackson T. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 2009, 16:401-412.
83. O'Reilly K.E., Rojo F., She Q.B., Solit D., Mills G.B., Smith D., Lane H., Hofmann F., Hicklin D.J., Ludwig D.L., Baselga J., Rosen N. mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res. 2006, 66:1500-1508.
84. Ooi A., Inokuchi M., Harada S., Inazawa J., Tajiri R., Kitamura S.S., Ikeda H., Kawashima H., Dobashi Y. Gene amplification of ESR1 in breast cancers - fact or fiction? A fluorescence in situ hybridization and multiplex ligation-dependent probe amplification study. J.Pathol. 2012, 227:8-16.
85. Osborne C.K., Bardou V., Hopp T.A., Chamness G.C., Hilsenbeck S.G., Fuqua S.A., Wong J., Allred D.C., Clark G.M., Schiff R. Role of the estrogen receptor coactivator AIB1 (SRC-3) and HER-2/neu in tamoxifen resistance in breast cancer. J.Natl. Cancer Inst. 2003, 95:353-361.
86. Osborne C.K., Schiff R. Mechanisms of endocrine resistance in breast cancer. Annu. Rev. Med. 2011, 62:233-247.
87. Ou Si B.Y., Camidge D.R., Riely G.J., Salgia R., Shapiro G., Solomon B.J., Engelman J.A., Kwak E.L., Clark J.W., Tye L., Wilner K.D., Stephenson P., Varella-Garcia M., Bergethon K., Iafrate A.J., Shaw A.T. Efficacy and safety of crizotinib in patients with advanced ROS1-rearranged non-small cell lung cancer (NSCLC). J.Clin. Oncol. 2013, 13(Suppl.). abstr 8032.
88. Poulikakos P.I., Persaud Y., Janakiraman M., Kong X., Ng C., Moriceau G., Shi H., Atefi M., Titz B., Gabay M.T., Salton M., Dahlman K.B., Tadi M., Wargo J.A., Flaherty K.T., Kelley M.C., Misteli T., Chapman P.B., Sosman J.A., Graeber T.G., Ribas A., Lo R.S., Rosen N., Solit D.B. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature 2011, 480:387-390.
89. Prahallad A., Sun C., Huang S., Di Nicolantonio F., Salazar R., Zecchin D., Beijersbergen R.L., Bardelli A., Bernards R. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature 2012, 483:100-103.
90. Rizzo P., Miao H., D'Souza G., Osipo C., Song L.L., Yun J., Zhao H., Mascarenhas J., Wyatt D., Antico G., Hao L., Yao K., Rajan P., Hicks C., Siziopikou K., Selvaggi S., Bashir A., Bhandari D., Marchese A., Lendahl U., Qin J.Z., Tonetti D.A., Albain K., Nickoloff B.J., Miele L. Cross-talk between notch and the estrogen receptor in breast cancer suggests novel therapeutic approaches. Cancer Res. 2008, 68:5226-5235.
91. Robinson D.R., Wu Y.M., Vats P., Su F., Lonigro R.J., Cao X., Kalyana-Sundaram S., Wang R., Ning Y., Hodges L., Gursky A., Siddiqui J., Tomlins S.A., Roychowdhury S., Pienta K.J., Kim S.Y., Roberts J.S., Rae J.M., Van Poznak C.H., Hayes D.F., Chugh R., Kunju L.P., Talpaz M., Schott A.F., Chinnaiyan A.M. Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nat. Genet. 2013, 45:1446-1451.
92. Sakamoto H., Tsukaguchi T., Hiroshima S., Kodama T., Kobayashi T., Fukami T.A., Oikawa N., Tsukuda T., Ishii N., Aoki Y. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell 2011, 19:679-690.
93. Salt M.B., Bandyopadhyay S., McCormick F. Epithelial-to-mesenchymal transition rewires the molecular path to PI3K-dependent proliferation. Cancer Discov. 2014, 4:186-199.
94. Sasaki T., Okuda K., Zheng W., Butrynski J., Capelletti M., Wang L., Gray N.S., Wilner K., Christensen J.G., Demetri G., Shapiro G.I., Rodig S.J., Eck M.J., Janne P.A. The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res. 2010, 70:10038-10043.
95. Scaltriti M., Verma C., Guzman M., Jimenez J., Parra J.L., Pedersen K., Smith D.J., Landolfi S., Ramon y Cajal S., Arribas J., Baselga J. Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity. Oncogene 2009, 28:803-814.
96. Sequist L.V., Waltman B.A., Dias-Santagata D., Digumarthy S., Turke A.B., Fidias P., Bergethon K., Shaw A.T., Gettinger S., Cosper A.K., Akhavanfard S., Heist R.S., Temel J., Christensen J.G., Wain J.C., Lynch T.J., Vernovsky K., Mark E.J., Lanuti M., Iafrate A.J., Mino-Kenudson M., Engelman J.A. Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Sci. Transl. Med. 2011, 3:75ra26.
97. Shaw A.T., Kim D.W., Nakagawa K., Seto T., Crino L., Ahn M.J., De Pas T., Besse B., Solomon B.J., Blackhall F., Wu Y.L., Thomas M., O'Byrne K.J., Moro-Sibilot D., Camidge D.R., Mok T., Hirsh V., Riely G.J., Iyer S., Tassell V., Polli A., Wilner K.D., Janne P.A. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N.Engl. J. Med. 2013, 368:2385-2394.
98. Shi H., Hugo W., Kong X., Hong A., Koya R.C., Moriceau G., Chodon T., Guo R., Johnson D.B., Dahlman K.B., Kelley M.C., Kefford R.F., Chmielowski B., Glaspy J.A., Sosman J.A., van Baren N., Long G.V., Ribas A., Lo R.S. Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy. Cancer Discov. 2014, 4:80-93.
99. Shi H., Moriceau G., Kong X., Lee M.K., Lee H., Koya R.C., Ng C., Chodon T., Scolyer R.A., Dahlman K.B., Sosman J.A., Kefford R.F., Long G.V., Nelson S.F., Ribas A., Lo R.S. Melanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance. Nat. Commun. 2012, 3:724.
100. Shi L., Dong B., Li Z., Lu Y., Ouyang T., Li J., Wang T., Fan Z., Fan T., Lin B., Wang Z., Xie Y. Expression of ER-{alpha}36, a novel variant of estrogen receptor {alpha}, and resistance to tamoxifen treatment in breast cancer. J.Clin. Oncol. 2009, 27:3423-3429.
101. Shiau A.K., Barstad D., Loria P.M., Cheng L., Kushner P.J., Agard D.A., Greene G.L. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell 1998, 95:927-937.
102. Singh M.S., Francis P.A., Michael M. Tamoxifen, cytochrome P450 genes and breast cancer clinical outcomes. Breast 2011, 20:111-118.
103. Smith I.E., Dowsett M. Aromatase inhibitors in breast cancer. N.Engl. J. Med. 2003, 348:2431-2442.
104. Sosman J.A., Kim K.B., Schuchter L., Gonzalez R., Pavlick A.C., Weber J.S., McArthur G.A., Hutson T.E., Moschos S.J., Flaherty K.T., Hersey P., Kefford R., Lawrence D., Puzanov I., Lewis K.D., Amaravadi R.K., Chmielowski B., Lawrence H.J., Shyr Y., Ye F., Li J., Nolop K.B., Lee R.J., Joe A.K., Ribas A. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N.Engl. J. Med. 2012, 366:707-714.
105. Straussman R., Morikawa T., Shee K., Barzily-Rokni M., Qian Z.R., Du J., Davis A., Mongare M.M., Gould J., Frederick D.T., Cooper Z.A., Chapman P.B., Solit D.B., Ribas A., Lo R.S., Flaherty K.T., Ogino S., Wargo J.A., Golub T.R. Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion. Nature 2012, 487:500-504.
106. Sun C., Hobor S., Bertotti A., Zecchin D., Huang S., Galimi F., Cottino F., Prahallad A., Grernrum W., Tzani A., Schlicker A., Wessels L.F., Smit E.F., Thunnissen E., Halonen P., Lieftink C., Beijersbergen R.L., Di Nicolantonio F., Bardelli A., Trusolino L., Bernards R. Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3. Cell Rep. 2014, 7:86-93.
107. Sun C., Wang L., Huang S., Heynen G.J., Prahallad A., Robert C., Haanen J., Blank C., Wesseling J., Willems S.M., Zecchin D., Hobor S., Bajpe P.K., Lieftink C., Mateus C., Vagner S., Grernrum W., Hofland I., Schlicker A., Wessels L.F., Beijersbergen R.L., Bardelli A., Di Nicolantonio F., Eggermont A.M., Bernards R. Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma. Nature 2014, 508:118-122.
108. Swain S.M., Kim S.B., Cortes J., Ro J., Semiglazov V., Campone M., Ciruelos E., Ferrero J.M., Schneeweiss A., Knott A., Clark E., Ross G., Benyunes M.C., Baselga J. Pertuzumab, trastuzumab, and docetaxel for HER2-positive metastatic breast cancer (CLEOPATRA study): overall survival results from a randomised, double-blind, placebo-controlled, phase 3 study. Lancet Oncol. 2013, 14:461-471.
109. Takezawa K., Pirazzoli V., Arcila M.E., Nebhan C.A., Song X., de Stanchina E., Ohashi K., Janjigian Y.Y., Spitzler P.J., Melnick M.A., Riely G.J., Kris M.G., Miller V.A., Ladanyi M., Politi K., Pao W. HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation. Cancer Discov. 2012, 2:922-933.
110. Thomson S., Buck E., Petti F., Griffin G., Brown E., Ramnarine N., Iwata K.K., Gibson N., Haley J.D. Epithelial to mesenchymal transition is a determinant of sensitivity of non-small-cell lung carcinoma cell lines and xenografts to epidermal growth factor receptor inhibition. Cancer Res. 2005, 65:9455-9462.
111. Tolhurst R.S., Thomas R.S., Kyle F.J., Patel H., Periyasamy M., Photiou A., Thiruchelvam P.T., Lai C.F., Al-Sabbagh M., Fisher R.A., Barry S., Crnogorac-Jurcevic T., Martin L.A., Dowsett M., Charles Coombes R., Kamalati T., Ali S., Buluwela L. Transient over-expression of estrogen receptor-alpha in breast cancer cells promotes cell survival and estrogen-independent growth. Breast Cancer Res. Treat. 2011, 128:357-368.
112. Toy W., Shen Y., Won H., Green B., Sakr R.A., Will M., Li Z., Gala K., Fanning S., King T.A., Hudis C., Chen D., Taran T., Hortobagyi G., Greene G., Berger M., Baselga J., Chandarlapaty S. ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nat. Genet. 2013, 45:1439-1445.
113. Trunzer K., Pavlick A.C., Schuchter L., Gonzalez R., McArthur G.A., Hutson T.E., Moschos S.J., Flaherty K.T., Kim K.B., Weber J.S., Hersey P., Long G.V., Lawrence D., Ott P.A., Amaravadi R.K., Lewis K.D., Puzanov I., Lo R.S., Koehler A., Kockx M., Spleiss O., Schell-Steven A., Gilbert H.N., Cockey L., Bollag G., Lee R.J., Joe A.K., Sosman J.A., Ribas A. Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma. J.Clin. Oncol. 2013, 31:1767-1774.
114. Turke A.B., Zejnullahu K., Wu Y.L., Song Y., Dias-Santagata D., Lifshits E., Toschi L., Rogers A., Mok T., Sequist L., Lindeman N.I., Murphy C., Akhavanfard S., Yeap B.Y., Xiao Y., Capelletti M., Iafrate A.J., Lee C., Christensen J.G., Engelman J.A., Janne P.A. Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell 2010, 17:77-88.
115. Valtorta E., Misale S., Sartore-Bianchi A., Nagtegaal I.D., Paraf F., Lauricella C., Dimartino V., Hobor S., Jacobs B., Ercolani C., Lamba S., Scala E., Veronese S., Laurent-Puig P., Siena S., Tejpar S., Mottolese M., Punt C.J., Gambacorta M., Bardelli A., Di Nicolantonio F. KRAS gene amplification in colorectal cancer and impact on response to EGFR-targeted therapy. Int. J. Cancer 2013, 133:1259-1265.
116. Van Allen E.M., Wagle N., Sucker A., Treacy D.J., Johannessen C.M., Goetz E.M., Place C.S., Taylor-Weiner A., Whittaker S., Kryukov G.V., Hodis E., Rosenberg M., McKenna A., Cibulskis K., Farlow D., Zimmer L., Hillen U., Gutzmer R., Goldinger S.M., Ugurel S., Gogas H.J., Egberts F., Berking C., Trefzer U., Loquai C., Weide B., Hassel J.C., Gabriel S.B., Carter S.L., Getz G., Garraway L.A., Schadendorf D. The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov. 2014, 4:94-109.
117. van der Flier S., Brinkman A., Look M.P., Kok E.M., Meijer-van Gelder M.E., Klijn J.G., Dorssers L.C., Foekens J.A. Bcar1/p130Cas protein and primary breast cancer: prognosis and response to tamoxifen treatment. J.Natl. Cancer Inst. 2000, 92:120-127.
118. Villanueva J., Vultur A., Lee J.T., Somasundaram 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., Hayden J.E., Brown K.D., Laquerre S., McArthur G.A., Sosman J.A., Nathanson K.L., Herlyn M. 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 2010, 18:683-695.
119. Wagle N., Emery C., Berger M.F., Davis M.J., Sawyer A., Pochanard P., Kehoe S.M., Johannessen C.M., Macconaill L.E., Hahn W.C., Meyerson M., Garraway L.A. Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J.Clin. Oncol. 2011, 29:3085-3096.
120. Wagle N., Van Allen E.M., Treacy D.J., Frederick D.T., Cooper Z.A., Taylor-Weiner A., Rosenberg M., Goetz E.M., Sullivan R.J., Farlow D.N., Friedrich D.C., Anderka K., Perrin D., Johannessen C.M., McKenna A., Cibulskis K., Kryukov G., Hodis E., Lawrence D.P., Fisher S., Getz G., Gabriel S.B., Carter S.L., Flaherty K.T., Wargo J.A., Garraway L.A. MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition. Cancer Discov. 2014, 4:61-68.
121. Walter A.O., Sjin R.T., Haringsma H.J., Ohashi K., Sun J., Lee K., Dubrovskiy A., Labenski M., Zhu Z., Wang Z., Sheets M., St Martin T., Karp R., van Kalken D., Chaturvedi P., Niu D., Nacht M., Petter R.C., Westlin W., Lin K., Jaw-Tsai S., Raponi M., Van Dyke T., Etter J., Weaver Z., Pao W., Singh J., Simmons A.D., Harding T.C., Allen A. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013, 3:1404-1415.
122. Wang J., Jain S., Coombes C.R., Palmieri C. Fulvestrant in advanced breast cancer following tamoxifen and aromatase inhibition: a single center experience. Breast J. 2009, 15:247-253.
123. Weinstein I.B. Cancer. Addiction to oncogenes - the Achilles heal of cancer. Science 2002, 297:63-64.
124. Xia W., Gerard C.M., Liu L., Baudson N.M., Ory T.L., Spector N.L. Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene 2005, 24:6213-6221.
125. Yamnik R.L., Holz M.K. mTOR/S6K1 and MAPK/RSK signaling pathways coordinately regulate estrogen receptor alpha serine 167 phosphorylation. FEBS Lett. 2010, 584:124-128.
126. Yano S., Nakataki E., Ohtsuka S., Inayama M., Tomimoto H., Edakuni N., Kakiuchi S., Nishikubo N., Muguruma H., Sone S. Retreatment of lung adenocarcinoma patients with gefitinib who had experienced favorable results from their initial treatment with this selective epidermal growth factor receptor inhibitor: a report of three cases. Oncol. Res. 2005, 15:107-111.
127. Yauch R.L., Januario T., Eberhard D.A., Cavet G., Zhu W., Fu L., Pham T.Q., Soriano R., Stinson J., Seshagiri S., Modrusan Z., Lin C.Y., O'Neill V., Amler L.C. Epithelial versus mesenchymal phenotype determines invitro sensitivity and predicts clinical activity of erlotinib in lung cancer patients. Clin. Cancer Res. 2005, 11:8686-8698.
128. Yoo C., Kim S.B., Ahn J.H., Jung K.H., Ahn Y., Gong G., Kim H.H., Kim H.J., Son B.H., Ahn S.H. Efficacy of fulvestrant in heavily pretreated postmenopausal women with advanced breast cancer: a preliminary report. J.Breast Cancer 2011, 14:135-139.
129. Zhou W., Ercan D., Chen L., Yun C.H., Li D., Capelletti M., Cortot A.B., Chirieac L., Iacob R.E., Padera R., Engen J.R., Wong K.K., Eck M.J., Gray N.S., Janne P.A. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009, 462:1070-1074.