REFERENCES
1. Arora A, Scholar EM. Role of tyrosine kinase inhibitors in cancer therapy. J Pharmacol Exp Ther 2005;315:971-9.
2. Hollenberg MD. Tyrosine kinase-mediated signal transduction pathways and the actions of polypeptide growth factors and G-protein-coupled agonists in smooth muscle. Mol Cell Biochem 1995;149-150:77-85.
3. Anafi M, Gazit A, Zehavi A, Ben-Neriah Y, Levitzki A. Tyrphostin-induced inhibition of p210bcr-abl tyrosine kinase activity induces K562 to differentiate. Blood 1993;82:3524-9.
4. Meydan N, Grunberger T, Dadi H, Shahar M, Arpaia E, et al. Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor. Nature 1996;379:645-8.
5. Oxnard GR, Lo PC, Nishino M, Dahlberg SE, Lindeman NI, et al. Natural history and molecular characteristics of lung cancers harboring EGFR exon 20 insertions. J Thorac Oncol 2013;8:179-84.
6. Arcila ME, Nafa K, Chaft JE, Rekhtman N, Lau C, et al. EGFR exon 20 insertion mutations in lung adenocarcinomas: prevalence, molecular heterogeneity, and clinicopathologic characteristics. Mol Cancer Ther 2013;12:220-9.
7. Yang JC, Sequist LV, Geater SL, Tsai CM, Mok TS, et al. Clinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6. Lancet Oncol 2015;16:830-8.
8. Sequist LV, Waltman BA, Dias-Santagata D, Digumarthy S, Turke AB, et al. Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Sci Transl Med 2011;3:75ra26.
9. Campo M, Gerber D, Gainor JF, Heist RS, Temel JS, et al. Acquired resistance to first-line afatinib and the challenges of prearranged progression biopsies. J Thorac Oncol 2016;11:2022-6.
10. Yu HA, Arcila ME, Rekhtman N, Sima CS, Zakowski MF, 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;19:2240-7.
11. Holohan C, Van Schaeybroeck S, Longley DB, Johnston PG. Cancer drug resistance: an evolving paradigm. Nat Rev Cancer 2013;13:714-26.
14. Druker BJ, Tamura S, Buchdunger E, Ohno S, Segal GM, et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 1996;2:561-6.
15. Taylor ST, Hickman JA, Dive C. Epigenetic determinants of resistance to etoposide regulation of Bcl-X(L) and bax by tumor microenvironmental factors. J Natl Cancer Inst 2000;92:18-23.
18. Paul MK, Mukhopadhyay AK. Tyrosine kinase - role and significance in cancer. Int J Med Sci 2004;1:101-15.
19. Lisovsky M, Estrov Z, Zhang X, Consoli U, Sanchez-Williams G, et al. Flt3 ligand stimulates proliferation and inhibits apoptosis of acute myeloid leukemia cells: regulation of Bcl-2 and Bax. Blood 1996;88:3987-97.
20. Testa U, Pelosi E. The impact of FLT3 mutations on the development of acute myeloid leukemias. Leuk Res Treatment 2013;2013:275760.
22. Vogelstein B, Papadopoulos N, Velculescu VE, Zhou S, Diaz LA Jr, et al. Cancer genome landscapes. Science 2013;339:1546-58.
23. Carraway KL, Sweeney C. EGF receptor activation by heterologous mechanisms. Cancer Cell 2002;1:405-6.
24. Groffen J, Stephenson JR, Heisterkamp N, de Klein A, Bartram CR, et al. Philadelphia chromosomal breakpoints are clustered within a limited region, bcr, on chromosome 22. Cell 1984;36:93-9.
25. Singh AB, Harris RC. Autocrine, paracrine and juxtacrine signaling by EGFR ligands. Cell Signal 2005;17:1183-93.
26. Kentsis A, Reed C, Rice KL, Sanda T, Rodig SJ, et al. Autocrine activation of the MET receptor tyrosine kinase in acute myeloid leukemia. Nat Med 2012;18:1118-22.
27. Krystal GW, Hines SJ, Organ CP. Autocrine growth of small cell lung cancer mediated by coexpression of c-kit and stem cell factor. Cancer Res 1996;56:370-6.
28. O’Brien SG, Guilhot F, Larson RA, Gathmann I, Baccarani M, et al. Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med 2003;348:994-1004.
29. Kris MG, Natale RB, Herbst RS, Lynch T, Prager D, et al. A phase II trial of ZD1839 (Iressa) in advanced non-small cell lung cancer (NSCLC) patients who had failed platinum- and docetaxel-based regimens (IDEAL 2). Proc Am Soc Clin Oncol 2002;21.
30. Fukuoka M, Yano S, Giaccone G, Tamura T, Nakagawa K, et al. Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer. J Clin Oncol 2003;21:2237-46.
31. Hidalgo M, Siu LL, Nemunaitis J, Rizzo J, Hammond LA, et al. Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J Clin Oncol 2001;19:3267-79.
32. Moore MJ, da Cunha Santos G, Kamel-Reid S, Chin K, Tu D, et al. The relationship of K-ras mutations and EGFR gene copy number to outcome in patients treated with Erlotinib on national cancer institute of canada clinical trials group trial study PA.3. J Clin Oncol 2007;25:4521.
33. Moore MJ, Goldstein D, Hamm J, Figer A, Hecht JR, et al. Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the national cancer institute of canada clinical trials group. J Clin Oncol 2007;25:1960-6.
34. de Claro RA, McGinn KM, Verdun N, Lee SL, Chiu HJ, et al. CCR perspectives in drug approval FDA approval: ibrutinib for patients with previously treated mantle cell lymphoma and previously treated chronic lymphocytic leukemia CME staff planners’ disclosures acknowledgment of financial or other support. Clin Cancer Res 2015;21:3586-90.
35. Castillo JJ, Palomba ML, Advani R, Treon SP. Ibrutinib in waldenström macroglobulinemia: latest evidence and clinical experience. Ther Adv Hematol 2016;7:179-86.
36. Sun L, Liang C, Shirazian S, Zhou Y, Miller T, et al. Discovery of 5-[5-Fluoro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem 2003;46:1116-9.
37. Shah NP, Sawyers CL. Mechanisms of resistance to STI571 in philadelphia chromosome-associated leukemias. Oncogene 2003;22:7389-95.
38. Druker BJ, Guilhot F, O’Brien SG, Gathmann I, Kantarjian H, et al. Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 2006;355:2408-17.
39. Shah NP, Tran C, Lee FY, Chen P, Norris D, et al. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 2004;305:399-401.
40. Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, et al. Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual src/abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem 2004;47:6658-61.
41. Grüllich C. Cabozantinib: a met, ret, and VEGFR2 tyrosine kinase inhibitor. Recent Results Cancer Res 2014;201:207-14.
42. U.S. Food and Drug Administration. FDA grants regular approval to cabometyx for first-line treatment of advanced renal cell carcinoma. Available from: https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm589842. [Last assessed on 27 Mar 2019].
43. Zhou Y, Zhang Y, Zou H, Cai N, Chen X, et al. The multi-targeted tyrosine kinase inhibitor vandetanib plays a bifunctional role in non-small cell lung cancer cells. Sci Rep 2015;5:8629.
44. Morabito A, Piccirillo MC, Falasconi F, De Feo G, Del Giudice A, et al. Vandetanib (ZD6474), a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) tyrosine kinases: current status and future directions. Oncologist 2009;14:378-90.
45. Lugowska I, Koseła-Paterczyk H, Kozak K, Rutkowski P. Trametinib: a MEK inhibitor for management of metastatic melanoma. Onco Targets Ther 2015;8:2251-9.
46. Verstovsek S, Kantarjian H, Mesa RA, Pardanani AD, Cortes-Franco J, et al. Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis. N Engl J Med 2010;363:1117-27.
47. Verstovsek S, Mesa RA, Gotlib J, Levy RS, Gupta V, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med 2012;366:799-807.
48. Harrison C, Kiladjian JJ, Al-Ali HK, Gisslinger H, Waltzman R, et al. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med 2012;366:787-98.
49. Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, et al. Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and board-spectrum potency against ALK-resistant mutations. J Med Chem 2014;57:4720-44.
50. Animal Cell Technology Industrial Platform. Monoclonal antibodies approved by the EMA and FDA for therapeutic use (status 2017). Available from: http://www.actip.org/products/monoclonal-antibodies-approved-by-the-ema-and-fda-for-therapeutic-use. [Last assessed on 27 Mar 2019].
51. Liu MZ, McLeod HL, He FZ, Chen XP, Zhou HH, et al. Epigenetic perspectives on cancer chemotherapy response. Pharmacogenomics 2014;15:699-715.
52. Strauss J, Figg WD. Using epigenetic therapy to overcome chemotherapy resistance. Anticancer Res 2016;36:1-4.
53. Bannister AJ, Kouzarides T. Regulation of chromatin by histone modifications. Cell Res 2011;21:381-95.
54. Kharkar VJ, Ast A, Gupta S, Sharma S. LSD2/KDM1B/AOF1 and human cancer pathways: a literature review. Cancer Stud Ther 2016;1:1-5.
55. Greer EL, Shi Y. Histone methylation: a dynamic mark in health, disease and inheritance. Nat Rev Genet 2012;13:343-57.
56. Suzuki T, Terashima M, Tange S, Ishimura A. Roles of histone methyl-modifying enzymes in development and progression of cancer. Cancer Sci 2013;104:795-800.
57. Rotili D, Mai A. Targeting histone demethylases: a new avenue for the fight against cancer. Genes Cancer 2011;2:663-79.
58. Tian X, Zhang S, Liu HM, Zhang YB, Blair CA, et al. Histone lysine-specific methyltransferases and demethylases in carcinogenesis: new targets for cancer therapy and prevention. Curr Cancer Drug Targets 2013;10:558-79.
59. Thinnes CC, England KS, Kawamura A, Chowdhury R, Schofield CJ, et al. Targeting histone lysine demethylases - progress, challenges, and the future. Biochim Biophys Acta 2014;1839:1416-32.
60. Fu X, Zhang P, Yu B. Advances toward LSD1 inhibitors for cancer therapy. Future Med Chem 2017;9:1227-42.
61. Kang MK, Mehrazarin S, Park NH, Wang CY. Epigenetic gene regulation by histone demethylases: emerging role in oncogenesis and inflammation. Oral Dis 2017;23:709-20.
62. Oh S, Janknecht R. Histone demethylase JMJD5 is essential for embryonic development. Biochem Biophys Res Commun 2012;420:61-5.
63. Strobl-Mazzulla PH, Sauka-Spengler T, Bronner-Fraser M. Histone demethylase JmjD2A regulates neural crest specification. Dev Celll 2010;19:460-8.
64. Black JC, Manning AL, Van Rechem C, Kim J, Ladd B, et al. KDM4A lysine demethylase induces site-specific copy gain and rereplication of regions amplified in tumors. Cell 2013;154:541-55.
65. Young LC, Hendzel MJ. The oncogenic potential of Jumonji D2 (JMJD2/KDM4) histone demethylase overexpression. Biochem Cell Biol 2013;91:369-77.
66. Young LC, McDonald DW, Hendzel MJ. Kdm4b histone demethylase is a DNA damage response protein and confers a survival advantage following γ-Irradiation. J Biol Chem 2013;288:21376-88.
67. Lu Y, Liu Y, Oeck S, Glazer PM. Hypoxia promotes resistance to EGFR inhibition in NSCLC cells via the histone demethylases, LSD1 and PLU-1. Mol Cancer Res 2018;16:1458-69.
68. Oral histone deacetylase inhibitor 4SC-202 in patients with advanced hematologic malignancies (TOPAS). Available from: https://clinicaltrials.gov/ct2/show/NCT01344707. [Last assessed on 27 Mar 2019].
69. European Medicines Agency. Clinical trials register - search for ORY-1001. Available from: https://www.clinicaltrialsregister.eu/ctr-search/search?query=ORY-1001. [Last assessed on 27 Mar 2019].
70. U.S. National Library of Medicine. Study of sensitization of Non-M3 AML blasts to ATRA by epigenetic treatment with tranylcypromine (TCP) (TRANSATRA). Available from: https://clinicaltrials.gov/ct2/show/NCT02717884. [Last assessed on 27 Mar 2019].
71. U.S. National Library of Medicine. Phase 1 study of TCP-ATRA for adult patients with AML and MDS (TCP-ATRA). Available from: https://clinicaltrials.gov/ct2/show/NCT02273102. [Last assessed on 27 Mar 2019].
72. Huang M, Chen C, Geng J, Han D, Wang T, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett 2017;398:12-21.
73. Hou J, Wu J, Dombkowski A, Zhang K, Holowatyj A, et al. Genomic amplification and a role in drug-resistance for the KDM5A histone demethylase in breast cancer. Am J Transl Res 2012;4:247-56.
74. Gale M, Sayegh J, Cao J, Norcia M, Gareiss P, et al. Screen-identified selective inhibitor of lysine demethylase 5A blocks cancer cell growth and drug resistance. Oncotarget 2016;7:39931-44.
75. Fahim Golestaneh A, Sun M, Schwager C, Tang Z, Macher-Goeppinger S, et al. Abstract 3254: discovery of histone demethylase KDM5C inactivation as a novel mechanism for tumors resistant to VEGF RTKi via genome-wide in-vivo RNAi. Cancer Res 2016;76:3254.
76. Zimmermannova O, Kanderova V, Kuzilkova D, Lund-Johansen F, Doktorova E, et al. Multilevel molecular profiling to dissect resistance to tyrosine kinase inhibitors in TEL/ABL positive acute lymphoblastic leukemia. Available from: https://www.linkos.cz/lekar-a-multidisciplinarni-tym/kongresy/po-kongresu/databaze-tuzemskych-onkologickych-konferencnich-abstrakt/multilevel-molecular-profiling-to-dissect-resistance-to-tyrosine-kinase-inhibito/. [Last assessed on 27 Mar 2019].
77. Sharma SV, Lee DY, Li B, Quinlan MP, Takahashi F, et al. A chromatin-mediated reversible drug-tolerant state in cancer cell subpopulations. Cell 2010;141:69-80.
78. Shibue T, Weinberg RA. EMT, CSCs, and drug resistance: the mechanistic link and clinical implications. Nat Rev Clin Oncol 2017;14:611-29.
79. Mohammad HP, Smitheman KN, Kamat CD, Soong D, Federowicz KE, et al. A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC. Cancer Cell 2015;28:57-69.
80. Liang Y, Vogel JL, Narayanan A, Peng H, Kristie TM. Inhibition of the histone demethylase LSD1 blocks α-herpesvirus lytic replication and reactivation from latency. Nat Med 2009;15:1312-7.
81. Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SGT, et al. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia 2014;28:2155-64.