Mechanisms of resistance to EGFR tyrosine kinase inhibitors

Acta Pharmaceutica Sinica B

Volumn 5, Issue 5, 2015, Pages 390-401

  Huang, Lihua ^a   Fu, Liwu ^a  

^a SUN YAT SEN UNIVERSITY   (China)

Author keywords

EGFR; Mechanisms; Resistance; TKIs

Indexed keywords

AFATINIB; B RAF KINASE; BETA1 INTEGRIN; BIM PROTEIN; CRK LIKE PROTEIN; CYCLIN D1; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR 3; EPIDERMAL GROWTH FACTOR RECEPTOR 4; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; FIBROBLAST GROWTH FACTOR 2; FIBROBLAST GROWTH FACTOR RECEPTOR 2; FIBROBLAST GROWTH FACTOR RECEPTOR 3; GEFITINIB; HEAT SHOCK PROTEIN 90; INTERLEUKIN 6; KERATINOCYTE GROWTH FACTOR; LAPATINIB; NEUROFIBROMIN; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PHOSPHATIDYLINOSITOL 4,5 BISPHOSPHATE 3 KINASE; PLATELET DERIVED GROWTH FACTOR; PLATELET DERIVED GROWTH FACTOR BETA RECEPTOR; SCATTER FACTOR RECEPTOR; SOMATOMEDIN RECEPTOR; UNINDEXED DRUG; VASCULOTROPIN; VASCULOTROPIN RECEPTOR 1; VASCULOTROPIN RECEPTOR 2;

ALK GENE; AMINO ACID SUBSTITUTION; APOPTOSIS; BINDING AFFINITY; BRAF GENE; C MET GENE; CELL MIGRATION; CELL PROLIFERATION; CELL TRANSFORMATION; CYTOKINE RELEASE; DNA POLYMORPHISM; DRUG RESISTANCE; EGFR GENE; EML4 ALK FUSION GENE; EPITHELIAL MESENCHYMAL TRANSITION; FUSION GENE; GENE AMPLIFICATION; GENE MUTATION; HUMAN; ONCOGENE K RAS; PIK3CA GENE; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN DEGRADATION; PROTEIN DEPLETION; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; PROTEIN PROTEIN INTERACTION; REVIEW; UPREGULATION;

EID: 84947202381     PISSN: 22113835     EISSN: 22113843     Source Type: Journal    
DOI: 10.1016/j.apsb.2015.07.001     Document Type: Review

References (96)

1. Ciardiello F., Tortora G. EGFR antagonists in cancer treatment. N Engl J Med 2008, 358:1160-1174.
2. Bethune G., Bethune D., Ridgway N., Xu Z. Epidermal growth factor receptor (EGFR) in lung cancer: an overview and update. J Thorac Dis 2010, 2:48-51.
3. Yu H.A., Arcila M.E., Rekhtman N., Sima C.S., Zakowski M.F., Pao W., et al. Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers. Clin Cancer Res 2013, 19:2240-2247.
4. Kobayashi S., Boggon T.J., Dayaram T., Jänne P.A., Kocher O., Meyerson M., et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 2005, 352:786-792.
5. Yun C.H., Mengwasser K.E., Toms A.V., Woo M.S., Greulich H., Wong K.K., et al. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A 2008, 105:2070-2075.
6. Ma C., Wei S., Song Y. T790M and acquired resistance of EGFR TKI: a literature review of clinical reports. J Thorac Dis 2011, 3:10-18.
7. Fujita Y., Suda K., Kimura H., Matsumoto K., Arao T., Nagai T., et al. Highly sensitive detection of EGFR T790M mutation using colony hybridization predicts favorable prognosis of patients with lung cancer harboring activating EGFR mutation. J Thorac Oncol 2012, 7:1640-1644.
8. Su K.Y., Chen H.Y., Li K.C., Kuo M.L., Yang J.C., Chan W.K., et al. Pretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancer. J Clin Oncol 2012, 30:433-440.
9. Suda K., Onozato R., Yatabe Y., Mitsudomi T. EGFR T790M mutation: a double role in lung cancer cell survival?. J Thorac Oncol 2009, 4:1-4.
10. Hong Y.S., Jang W.J., Chun K.S., Jeong C.H. Hsp90 inhibition by WK88-1 potently suppresses the growth of gefitinib-resistant H1975 cells harboring the T790M mutation in EGFR. Oncol Rep 2014, 31:2619-2624.
11. Smith D.L., Acquaviva J., Sequeira M., Jimenez J.P., Zhang C., Sang J., et al. The HSP90 inhibitor ganetespib potentiates the antitumor activity of EGFR tyrosine kinase inhibition in mutant and wild-type non-small cell lung cancer. Target Oncol 2015, 10:235-245.
12. Costa D.B., Halmos B., Kumar A., Schumer S.T., Huberman M.S., Boggon T.J., et al. BIM mediates EGFR tyrosine kinase inhibitor-induced apoptosis in lung cancers with oncogenic EGFR mutations. PLoS Med 2007, 4:1669-1679.
13. Toyooka S., Date H., Uchida A., Kiura K., Takata M. The epidermal growth factor receptor D761Y mutation and effect of tyrosine kinase inhibitor. Clin Cancer Res 2007, 13:3431.
14. Bean J., Riely G.J., Balak M., Marks J.L., Ladanyi M., Miller V.A., et al. 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 2008, 14:7519-7525.
15. Woo H.S., Ahn H.K., Lee H.Y., Park I., Kim Y.S., Hong J., et al. Epidermal growth factor receptor (EGFR) exon 20 mutations in non-small-cell lung cancer and resistance to EGFR-tyrosine kinase inhibitors. Invest New Drugs 2014, 32:1311-1315.
16. Khan N.A., Mirshahidi S., Mirshahidi H.R. A novel insertion mutation on exon 20 of epidermal growth factor receptor, conferring resistance to erlotinib. Case Rep Oncol 2014, 7:491-496.
17. Landi L., Cappuzzo F. HER2 and lung cancer. Expert Rev Anticancer Ther 2013, 13:1219-1228.
18. Nishida Y., Kuwata T., Nitta H., Dennis E., Aizawa M., Kinoshita T., et al. A novel gene-protein assay for evaluating HER2 status in gastric cancer: simultaneous analyses of HER2 protein overexpression and gene amplification reveal intratumoral heterogeneity. Gastric Cancer 2014 Jun 11, 10.1007/s10120-014-0394-7.
19. Engelman J.A., Zejnullahu K., Mitsudomi T., Song Y., Hyland C., Park J.O., et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007, 316:1039-1043.
20. + breast cancer models. Breast Cancer Res 2013, 15:R85.
21. Nakata S., Tanaka H., Ito Y., Hara M., Fujita M., Kondo E., et al. Deficient HER3 expression in poorly-differentiated colorectal cancer cells enhances gefitinib sensitivity. Int J Oncol 2014, 45:1583-1593.
22. Schoeberl B., Faber A.C., Li D., Liang M.C., Crosby K., Onsum M., et al. An ErbB3 antibody, MM-121, is active in cancers with ligand-dependent activation. Cancer Res 2010, 70:2485-2494.
23. Kubo T., Yamamoto H., Lockwood W.W., Valencia I., Soh J., Peyton M., et al. MET gene amplification or EGFR mutation activate MET in lung cancers untreated with EGFR tyrosine kinase inhibitors. Int J Cancer 2009, 124:1778-1784.
24. Yano S., Wang W., Li Q., Matsumoto K., Sakurama H., Nakamura T., et al. Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations. Cancer Res 2008, 68:9479-9487.
25. Mueller K.L., Madden J.M., Zoratti G.L., Kuperwasser C., List K., Boerner J.L. Fibroblast-secreted hepatocyte growth factor mediates epidermal growth factor receptor tyrosine kinase inhibitor resistance in triple-negative breast cancers through paracrine activation of Met. Breast Cancer Res 2012, 14:R104.
26. Guix M., Faber A.C., Wang S.E., Olivares M.G., Song Y., Qu S., et al. Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins. J Clin Invest 2008, 118:2609-2619.
27. Peled N., Wynes M.W., Ikeda N., Ohira T., Yoshida K., Qian J. Insulin-like growth factor-1 receptor (IGF-1R) as a biomarker for resistance to the tyrosine kinase inhibitor gefitinib in non-small cell lung cancer. Cell Oncol 2013, 36:277-288.
28. Jameson M.J., Taniguchi L.E., VanKoevering K.K., Stuart M.M., Francom C.R., Mendez R.E., et al. Activation of the insulin-like growth factor-1 receptor alters p27 regulation by the epidermal growth factor receptor in oral squamous carcinoma cells. J Oral Pathol Med 2013, 42:332-338.
29. Ballas M.S., Chachoua A. Rationale for targeting VEGF, FGF, and PDGF for the treatment of NSCLC. Onco Targets Ther 2011, 4:43-58.
30. Chatterjee S., Heukamp L.C., Siobal M., Schöttle J., Wieczorek C., Peifer M., et al. Tumor VEGF:VEGFR2 autocrine feed-forward loop triggers angiogenesis in lung cancer. J Clin Invest 2013, 123:1732-1740.
31. Bianco R., Rosa R., Damiano V., Daniele G., Gelardi T., Garofalo S., et al. Vascular endothelial growth factor receptor-1 contributes to resistance to anti-epidermal growth factor receptor drugs in human cancer cells. Clin Cancer Res 2008, 14:5069-5080.
32. Ware K.E., Marshall M.E., Heasley L.R., Marek L., Hinz T.K., Hercule P., et al. Rapidly acquired resistance to EGFR tyrosine kinase inhibitors in NSCLC cell lines through de-repression of FGFR2 and FGFR3 expression. PLoS One 2010, 5:e14117.
33. Azuma K., Kawahara A., Sonoda K., Nakashima K., Tashiro K., Watari K., et al. FGFR1 activation is an escape mechanism in human lung cancer cells resistant to afatinib, a pan-EGFR family kinase inhibitor. Oncotarget 2014, 5:5908-5919.
34. Akhavan D., Pourzia A.L., Nourian A.A., Williams K.J., Nathanson D., Babic I., et al. De-repression of PDGFRβ transcription promotes acquired resistance to EGFR tyrosine kinase inhibitors in glioblastoma patients. Cancer Discov 2013, 3:534-547.
35. Bonavia R., Inda M.M., Vandenberg S., Cheng S.Y., Nagane M., Hadwiger P., et al. EGFRvIII promotes glioma angiogenesis and growth through the NF-κB, interleukin-8 pathway. Oncogene 2012, 31:4054-4066.
36. Katanasaka Y., Kodera Y., Kitamura Y., Morimoto T., Tamura T., Koizumi F. Epidermal growth factor receptor variant type III markedly accelerates angiogenesis and tumor growth via inducing c-myc mediated angiopoietin-like 4 expression in malignant glioma. Mol Cancer 2013, 12:31.
37. Zhang Z., Lee J.C., Lin L., Olivas V., Au V., LaFramboise T., et al. Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer. Nat Genet 2012, 44:852-860.
38. Lee Y., Lee M., Kim S. GAS6 induces cancer cell migration and epithelial-mesenchymal transition through upregulation of MAPK and Slug. Biochem Biophys Res Commun 2013, 434:8-14.
39. Kim S.M., Kwon O.J., Hong Y.K., Kim J.H., Solca F., Ha S.J., et al. Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutation. Mol Cancer Ther 2012, 11:2254-2264.
40. Ishiguro Y., Ishiguro H., Miyamoto H. Epidermal growth factor receptor tyrosine kinase inhibition up-regulates interleukin-6 in cancer cells and induces subsequent development of interstitial pneumonia. Oncotarget 2013, 4:550-559.
41. Wang Y., van Boxel-Dezaire A.H., Cheon H., Yang J., Stark G.R. STAT3 activation in response to IL-6 is prolonged by the binding of IL-6 receptor to EGF receptor. Proc Natl Acad Sci U S A 2013, 110:16975-16980.
42. Yao Z., Fenoglio S., Gao D.C., Camiolo M., Stiles B., Lindsted T., et al. TGF-β IL-6 axis mediates selective and adaptive mechanisms of resistance to molecular targeted therapy in lung cancer. Proc Natl Acad Sci U S A 2010, 107:15535-15540.
43. Suda K., Mizuuchi H., Murakami I., Uramoto H., Tanaka F., Sato K., et al. CRKL amplification is rare as a mechanism for acquired resistance to kinase inhibitors in lung cancers with epidermal growth factor receptor mutation. Lung Cancer 2014, 85:147-151.
44. Cheung H.W., Du J., Boehm J.S., He F., Weir B.A., Wang X., et al. Amplification of CRKL induces transformation and epidermal growth factor receptor inhibitor resistance in human non-small cell lung cancers. Cancer Discov 2011, 1:608-625.
45. Lin F., Xie C.Y., Li Q.C., Dong Q.Z., Wang E.H., Wang Y. CRKL promotes lung cancer cell invasion through ERK-MMP9 pathway. Mol Carcinog 2015, 54 Suppl 1:E35-44.
46. Ju L., Zhou C., Li W., Yan L. Integrin beta1 over-expression associates with resistance to tyrosine kinase inhibitor gefitinib in non-small cell lung cancer. J Cell Biochem 2010, 111:1565-1574.
47. Huang C., Park C.C., Hilsenbeck S.G., Ward R., Rimawi M.F., Wang Y.C., et al. β1 Integrin mediates an alternative survival pathway in breast cancer cells resistant to lapatinib. Breast Cancer Res 2011, 13:R84.
48. Ju L., Zhou C. Association of integrin beta1 and c-MET in mediating EGFR TKI gefitinib resistance in non-small cell lung cancer. Cancer Cell Int 2013, 13:15.
49. Kanda R., Kawahara A., Watari K., Murakami Y., Sonoda K., Maeda M., et al. Erlotinib resistance in lung cancer cells mediated by integrin β1/Src/Akt-driven bypass signaling. Cancer Res 2013, 73:6243-6253.
50. Brown W.S., Wendt M.K. Integrin-mediated resistance to epidermal growth factor receptor-targeted therapy: an inflammatory situation. Breast Cancer Res 2014, 16:448.
51. Pao W., Wang T.Y., Riely G.J., Miller V.A., Pan Q., Ladanyi M., et al. KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib. PLoS Med 2005, 2:e17.
52. de Mello R.A., Marques D.S., Medeiros R., Araújo A.M. Epidermal growth factor receptor and K-RAS in non-small cell lung cancer-molecular pathways involved and targeted therapies. World J Clin Oncol 2011, 2:367-376.
53. Repasky G.A., Chenette E.J., Der C.J. Renewing the conspiracy theory debate: does RAF function alone to mediate RAS oncogenesis?. Trends Cell Biol 2004, 14:639-647.
54. Bidkhori G., Moeini A., Masoudi-Nejad A. Modeling of tumor progression in NSCLC and intrinsic resistance to TKI in loss of PTEN expression. PLoS One 2012, 7:e48004.
55. Sos M.L., Koker M., Weir B.A., Heynck S., Rabinovsky R., Zander T., et al. PTEN loss contributes to erlotinib resistance in EGFR-mutant lung cancer by activation of Akt and EGFR. Cancer Res 2009, 69:3256-3261.
56. Kim E.J., Jeong J.H., Bae S., Kang S., Kim C.H., Lim Y.B. mTOR inhibitors radiosensitize PTEN-deficient non-small-cell lung cancer cells harboring an EGFR activating mutation by inducing autophagy. J Cell Biochem 2013, 114:1248-1256.
57. Ohashi K., Sequist L.V., Arcila M.E., Moran T., Chmielecki J., Lin Y.L., et al. Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1. Proc Natl Acad Sci U S A 2012, 109:E2127-E2133.
58. Whyte D.B., Holbeck S.L. Correlation of PIK3CA mutations with gene expression and drug sensitivity in NCI-60 cell lines. Biochem Biophys Res Commun 2006, 340:469-475.
59. Wang L., Hu H., Pan Y., Wang R., Li Y., Shen L., et al. PIK3CA mutations frequently coexist with EGFR/KRAS mutations in non-small cell lung cancer and suggest poor prognosis in EGFR/KRAS wildtype subgroup. PLoS One 2014, 9:e88291.
60. Bruin E.C., Cowell C., Warne P.H., Jiang M., Saunders R.E., Melnick M.A., et al. Reduced NF1 expression confers resistance to EGFR inhibition in lung cancer. Cancer Discov 2014, 4:606-619. de.
61. Ng K.P., Hillmer A.M., Chuah C.T., Juan W.C., Ko T.K., Teo A.S., et al. A common BIM deletion polymorphism mediates intrinsic resistance and inferior responses to tyrosine kinase inhibitors in cancer. Nat Med 2012, 18:521-528.
62. Kiyota M., Kuroda J., Yamamoto-Sugitani M., Shimura Y., Nakayama R., Nagoshi H., et al. FTY720 induces apoptosis of chronic myelogenous leukemia cells via dual activation of BIM and BID and overcomes various types of resistance to tyrosine kinase inhibitors. Apoptosis 2013, 18:1437-1446.
63. Thiery J.P. Epithelial-mesenchymal transitions in tumour progression. Nat Rev Cancer 2002, 2:442-454.
64. Bae G.Y., Choi S.J., Lee J.S., Jo J., Lee J., Kim J., et al. Loss of E-cadherin activates EGFR-MEK/ERK signaling, which promotes invasion via the ZEB1/MMP2 axis in non-small cell lung cancer. Oncotarget 2013, 4:2512-2522.
65. Palena C., Hamilton D.H., Fernando R.I. Influence of IL-8 on the epithelial-mesenchymal transition and the tumor microenvironment. Future Oncol 2012, 8:713-722.
66. Xie M., He C.S., Wei S.H., Zhang L. Notch-1 contributes to epidermal growth factor receptor tyrosine kinase inhibitor acquired resistance in non-small cell lung cancer in vitro and in vivo. Eur J Cancer 2013, 49:3559-3572.
67. Capaccione K.M., Hong X., Morgan K.M., Liu W., Bishop J.M., Liu L., et al. Sox9 mediates Notch1-induced mesenchymal features in lung adenocarcinoma. Oncotarget 2014, 5:3636-3650.
68. Xu M.M., Mao G.X., Liu J., Li J.C., Huang H., Liu Y.F., et al. Low expression of the FoxO4 gene may contribute to the phenomenon of EMT in non-small cell lung cancer. Asian Pac J Cancer Prev 2014, 15:4013-4018.
69. Park K.S., Raffeld M., Moon Y.W., Xi L., Bianco C., Pham T., et al. CRIPTO1 expression in EGFR-mutant NSCLC elicits intrinsic EGFR-inhibitor resistance. J Clin Invest 2014, 124:3003-3015.
70. Wilson C., Nicholes K., Bustos D., Lin E., Song Q., Stephan J.P., et al. Overcoming EMT-associated resistance to anti-cancer drugs via Src/FAK pathway inhibition. Oncotarget 2014, 5:7328-7341.
71. Alam N., Gustafson K.S., Ladanyi M., Zakowski M.F., Kapoor A., Truskinovsky A.M., et al. Small-cell carcinoma with an epidermal growth factor receptor mutation in a never-smoker with gefitinib-responsive adenocarcinoma of the lung. Clin Lung Cancer 2010, 11:E1-E4.
72. Shi Z., Tiwari A.K., Shukla S., Robey R.W., Singh S., Kim I.W., et al. Sildenafil reverses ABCB1- and ABCG2-mediated chemotherapeutic drug resistance. Cancer Res 2011, 71:3029-3041.
73. Sodani K., Tiwari A.K., Singh S., Patel A., Xiao Z.J., Chen J.J., et al. GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. Biochem Pharmacol 2012, 83:1613-1622.
74. Soda M., Choi Y.L., Enomoto M., Takada S., Yamashita Y., Ishikawa S., et al. Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer. Nature 2007, 448:561-566.
75. Kwak E.L., Bang Y.J., Camidge D.R., Shaw A.T., Solomon B., Maki R.G., et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med 2010, 363:1693-1703.
76. Zhang X., Zhang S., Yang X., Yang J., Zhou Q., Yin L., et al. Fusion of EML4 and ALK is associated with development of lung adenocarcinomas lacking EGFR and KRAS mutations and is correlated with ALK expression. Mol Cancer 2010, 9:188.
77. Pearson R., Kolesar J.M. Targeted therapy for NSCLC: ALK inhibition. J Oncol Pharm Pract 2012, 18:271-274.
78. Yamada T., Takeuchi S., Nakade J., Kita K., Nakagawa T., Nanjo S., et al. Paracrine receptor activation by microenvironment triggers bypass survival signals and ALK inhibitor resistance in EML4-ALK lung cancer cells. Clin Cancer Res 2012, 18:3592-3602.
79. Sasaki T., Koivunen J., Ogino A., Yanagita M., Nikiforow S., Zheng W., et al. A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res 2011, 71:6051-6060.
80. Perez-Torres M., Guix M., Gonzalez A., Arteaga C.L. Epidermal growth factor receptor (EGFR) antibody down-regulates mutant receptors and inhibits tumors expressing EGFR mutations. J Biol Chem 2006, 281:40183-40192.
81. Walter A.O., Sjin R.T., Haringsma H.J., Ohashi K., Sun J., Lee K., et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov 2013, 3:1404-1415.
82. Cross D.A., Ashton S.E., Ghiorghiu S., Eberlein C., Nebhan C.A., Spitzler P.J., et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov 2014, 4:1046-1061.
83. Hoeflich K.P., Merchant M., Orr C., Chan J., Den Otter D., Berry L., et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res 2012, 72:210-219.
84. Hong Z., Cao X., Li N., Zhang Y., Lan L., Zhou Y., et al. Luteolin is effective in the non-small cell lung cancer model with L858R/T790M EGF receptor mutation and erlotinib resistance. Br J Pharmacol 2014, 171:2842-2853.
85. Qu G., Liu C., Sun B., Zhou C., Zhang Z., Wang P. Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation. Oncol Rep 2014, 32:341-347.
86. Kim S.M., Yun M.R., Hong Y.K., Solca F., Kim J.H., Kim H.J., et al. Glycolysis inhibition sensitizes non-small cell lung cancer with T790M mutation to irreversible EGFR inhibitors via translational suppression of Mcl-1 by AMPK activation. Mol Cancer Ther 2013, 12:2145-2156.
87. Engelman J.A., Zejnullahu K., Gale C.M., Lifshits E., Gonzales A.J., Shimamura T., et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res 2007, 67:11924-11932.
88. Nanjo S., Yamada T., Nishihara H., Takeuchi S., Sano T., Nakagawa T., et al. Ability of the Met kinase inhibitor crizotinib and new generation EGFR inhibitors to overcome resistance to EGFR inhibitors. PLoS One 2013, 8:e84700.
89. Graves E.E., Maity A., Le Q.T. The tumor microenvironment in non-small-cell lung cancer. Semin Radiat Oncol 2010, 20:156-163.
90. Nakade J., Takeuchi S., Nakagawa T., Ishikawa D., Sano T., Nanjo S., et al. Triple inhibition of EGFR, Met, and VEGF suppresses regrowth of HGF-triggered, erlotinib-resistant lung cancer harboring an EGFR mutation. J Thorac Oncol 2014, 9:775-783.
91. Sarkar S., Rajput S., Tripathi A.K., Mandal M. Targeted therapy against EGFR and VEGFR using ZD6474 enhances the therapeutic potential of UV-B phototherapy in breast cancer cells. Mol Cancer 2013, 12:122.
92. Song L., Smith M.A., Doshi P., Sasser K., Fulp W., Altiok S., et al. Antitumor efficacy of the anti-interleukin-6 (IL-6) antibody siltuximab in mouse xenograft models of lung cancer. J Thorac Oncol 2014, 9:974-982.
93. Rho J.K., Choi Y.J., Kim S.Y., Kim T.W., Choi E.K., Yoon S.J., et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res 2014, 74:253-262.
94. Hofmann I., Weiss A., Elain G., Schwaederle M., Sterker D., Romanet V., et al. K-RAS mutant pancreatic tumors show higher sensitivity to MEK than to PI3K inhibition in vivo. PLoS One 2012, 7:e44146.
95. Rutkowski P., Blank C. Dabrafenib for the treatment of BRAF V600-positive melanoma: a safety evaluation. Expert Opin Drug Saf 2014, 13:1249-1258.
96. Ren H., Zhao L., Li Y., Yue P., Deng X., Owonikoko T.K., et al. The PI3 kinase inhibitor NVP-BKM120 induces GSK3/FBXW7-dependent Mcl-1 degradation, contributing to induction of apoptosis and enhancement of TRAIL-induced apoptosis. Cancer Lett 2013, 338:229-238.