• Cancer Genome Atlas Research Network. 2014, Comprehensive molecular characterization of urothelial bladder carcinoma. Nature 507, 315-322. • Arao, T., Ueshima, K., Matsumoto, K., Nagai, T., Kimura, H., Hagiwara, S., Sakurai, T., Haji, S., Kanazawa, A., Hidaka, H., Iso, Y., Kubota, K., Shimada, M., Utsunomiya, T., Hirooka, M., Hiasa, Y., Toyoki, Y., Hakamada, K., Yasui, K., Kumada, T., Toyoda, H., Sato, S., Hisai, H., Kuzuya, T., Tsuchiya, K., Izumi, N., Arii, S., Nishio, K., Kudo, M., 2013. FGF3/FGF4 amplification and multiple lung metastases in responders to sorafenib in hepatocellular carcinoma. Hepatology 57, 1407-1415. • Arkenau H, S.M., Hollebecque A, Mathewson A, Lemech C, Landers D, Frewer P, et al., 2014. A phase 1 expansion cohort of the fibroblast growth factor receptor (FGFR) inhibitor AZD4547 in patients (pts) with advanced gastric (GC) and gastroesophageal (GOJ) cancer. J. Clin. Oncol. 32:5s, 2014 (suppl; abstr 2620). • Asaumi M, F.T., Hisamichi H, Iikubo K, Iwai Y, Kameda M, Kawamoto Y, Kuriwaki I, Miyasaka K, Moritomo H, Noda A, Okada H, Suzuki A, Suzuki T, Tokuzaki K, Tomiyama H, Tsunoyama K, 2013. Nitrogen-containing Aromatic Heterocyclic Compound, in: Astellas Pharma Inc., K.P.C., Ltd (Ed.). Astellas Pharma Inc., Kotobuki Pharm Co., Ltd. • Bae, J.H., Lew, E.D., Yuzawa, S., Tome, F., Lax, I., Schlessinger, J., 2009. The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site. Cell 138, 514-524. • Bahleda R, D.R., Adamo B, Gazzah A, Jeffrey R, Bob Zhong, Suso J, et al, 2014. Phase 1 study of JNJ-42756493, a pan-fibroblast growth factor receptor (FGFR) inhibitor, in patients with advanced solid tumors. J. Clin. Oncol. 32:5s, (suppl; abstr 2501). • Bang, Y.J., Van Cutsem, E., Feyereislova, A., Chung, H.C., Shen, L., Sawaki, A., Lordick, F., Ohtsu, A., Omuro, Y., Satoh, T., Aprile, G., Kulikov, E., Hill, J., Lehle, M., Ruschoff, J., Kang, Y.K., 2010. Trastuzumab in combination with chemotherapy versus chemotherapy alone for treatment of HER2-positive advanced gastric or gastro-oesophageal junction cancer (ToGA): a phase 3, open-label, randomised controlled trial. Lancet 376, 687- 697. • Beenken, A., Mohammadi, M., 2009. The FGF family: biology, pathophysiology and therapy. Nat Rev Drug Discov 8, 235-253. • Belov, A.A., Mohammadi, M., 2013. Molecular mechanisms of fibroblast growth factor signaling in physiology and pathology. Cold Spring Harb Perspect Biol 5. • Blundell, T.L., Sibanda, B.L., Sternberg, M.J., Thornton, J.M., 1987. Knowledge-based prediction of protein structures and the design of novel molecules. Nature 326, 347-352. • Bray, F., Ferlay, J., Soerjomataram, I., Siegel, R.L., Torre, L.A., Jemal, A., 2018. Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin 68, 394-424. • Brown, A.P., Courtney, C.L., King, L.M., Groom, S.C., Graziano, M.J., 2005. Cartilage dysplasia and tissue mineralization in the rat following administration of a FGF receptor tyrosine kinase inhibitor. Toxicol Pathol 33, 449-455. • Campbell, J.D., Alexandrov, A., Kim, J., Wala, J., Berger, A.H., Pedamallu, C.S., Shukla, S.A., Guo, G., Brooks, A.N., Murray, B.A., Imielinski, M., Hu, X., Ling, S., Akbani, R., Rosenberg, M., Cibulskis, C., Ramachandran, A., Collisson, E.A., Kwiatkowski, D.J., Lawrence, M.S., Weinstein, J.N., Verhaak, R.G., Wu, C.J., Hammerman, 54 P.S., Cherniack, A.D., Getz, G., Artyomov, M.N., Schreiber, R., Govindan, R., Meyerson, M., 2016. Distinct patterns of somatic genome alterations in lung adenocarcinomas and squamous cell carcinomas. Nat Genet 48, 607-616. • Chen, H., Ma, J., Li, W., Eliseenkova, A.V., Xu, C., Neubert, T.A., Miller, W.T., Mohammadi, M., 2007. A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases. Mol Cell 27, 717- 730. • Chen, H., Marsiglia, W.M., Cho, M.K., Huang, Z., Deng, J., Blais, S.P., Gai, W., Bhattacharya, S., Neubert, T.A., Traaseth, N.J., Mohammadi, M., 2017. Elucidation of a four-site allosteric network in fibroblast growth factor receptor tyrosine kinases. Elife 6. • Chen, H., Xu, C.F., Ma, J., Eliseenkova, A.V., Li, W., Pollock, P.M., Pitteloud, N., Miller, W.T., Neubert, T.A., Mohammadi, M., 2008. A crystallographic snapshot of tyrosine trans-phosphorylation in action. Proc Natl Acad Sci U S A 105, 19660-19665. • Cheng, A.L., Kang, Y.K., Chen, Z., Tsao, C.J., Qin, S., Kim, J.S., Luo, R., Feng, J., Ye, S., Yang, T.S., Xu, J., Sun, Y., Liang, H., Liu, J., Wang, J., Tak, W.Y., Pan, H., Burock, K., Zou, J., Voliotis, D., Guan, Z., 2009. Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, double-blind, placebo-controlled trial. Lancet Oncol 10, 25-34. • Chong, I.Y., Cunningham, D., Barber, L.J., Campbell, J., Chen, L., Kozarewa, I., Fenwick, K., Assiotis, I., Guettler, S., Garcia-Murillas, I., Awan, S., Lambros, M., Starling, N., Wotherspoon, A., Stamp, G., Gonzalez-deCastro, D., Benson, M., Chau, I., Hulkki, S., Nohadani, M., Eltahir, Z., Lemnrau, A., Orr, N., Rao, S., Lord, C.J., Ashworth, A., 2013. The genomic landscape of oesophagogastric junctional adenocarcinoma. J Pathol 231, 301- 310. • Cocco, E., Scaltriti, M., Drilon, A., 2018. NTRK fusion-positive cancers and TRK inhibitor therapy. Nat Rev Clin Oncol 15, 731-747. • Desnoyers, L.R., Pai, R., Ferrando, R.E., Hotzel, K., Le, T., Ross, J., Carano, R., D'Souza, A., Qing, J., Mohtashemi, I., Ashkenazi, A., French, D.M., 2008. Targeting FGF19 inhibits tumor growth in colon cancer xenograft and FGF19 transgenic hepatocellular carcinoma models. Oncogene 27, 85-97. • Dienstmann, R., Brana, I., Rodon, J., Tabernero, J., 2011. Toxicity as a biomarker of efficacy of molecular targeted therapies: focus on EGFR and VEGF inhibiting anticancer drugs. Oncologist 16, 1729-1740. • Doi, I., 1976. Establishment of a cell line and its clonal sublines from a patient with hepatoblastoma. Gan 67, 1-10. • Dor, I., Namba, M., Sato, J., 1975. Establishment and some biological characteristics of human hepatoma cell lines. Gan 66, 385-392. • French, D.M., Lin, B.C., Wang, M., Adams, C., Shek, T., Hotzel, K., Bolon, B., Ferrando, R., Blackmore, C., Schroeder, K., Rodriguez, L.A., Hristopoulos, M., Venook, R., Ashkenazi, A., Desnoyers, L.R., 2012. Targeting FGFR4 inhibits hepatocellular carcinoma in preclinical mouse models. PLoS One 7, e36713. • Fu, L., John, L.M., Adams, S.H., Yu, X.X., Tomlinson, E., Renz, M., Williams, P.M., Soriano, R., Corpuz, R., Moffat, B., Vandlen, R., Simmons, L., Foster, J., Stephan, J.P., Tsai, S.P., Stewart, T.A., 2004. Fibroblast growth factor 19 increases metabolic rate and reverses dietary and leptin-deficient diabetes. Endocrinology 145, 2594- 2603. • Futami, T., Okada, H., Kihara, R., Kawase, T., Nakayama, A., Suzuki, T., Kameda, M., Shindoh, N., Terasaka, T., Hirano, M., Kuromitsu, S., 2017. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of 55 FGF19-Expressing Hepatocellular Carcinoma. Mol Cancer Ther 16, 68-75. • Gallo, L.H., Nelson, K.N., Meyer, A.N., Donoghue, D.J., 2015. Functions of Fibroblast Growth Factor Receptors in cancer defined by novel translocations and mutations. Cytokine Growth Factor Rev 26, 425-449. • Gao, Q., Liang, W.W., Foltz, S.M., Mutharasu, G., Jayasinghe, R.G., Cao, S., Liao, W.W., Reynolds, S.M., Wyczalkowski, M.A., Yao, L., Yu, L., Sun, S.Q., Chen, K., Lazar, A.J., Fields, R.C., Wendl, M.C., Van Tine, B.A., Vij, R., Chen, F., Nykter, M., Shmulevich, I., Ding, L., 2018. Driver Fusions and Their Implications in the Development and Treatment of Human Cancers. Cell Rep 23, 227-238.e223. • Gavine, P.R., Mooney, L., Kilgour, E., Thomas, A.P., Al-Kadhimi, K., Beck, S., Rooney, C., Coleman, T., Baker, D., Mellor, M.J., Brooks, A.N., Klinowska, T., 2012. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res 72, 2045-2056. • Gu, Q., Zhang, B., Sun, H., Xu, Q., Tan, Y., Wang, G., Luo, Q., Xu, W., Yang, S., Li, J., Fu, J., Chen, L., Yuan, S., Liang, G., Ji, Q., Chen, S.H., Chan, C.C., Zhou, W., Xu, X., Wang, H., Fang, D.D., 2015. Genomic characterization of a large panel of patient-derived hepatocellular carcinoma xenograft tumor models for preclinical development. Oncotarget 6, 20160-20176. • Guagnano, V., Furet, P., Spanka, C., Bordas, V., Le Douget, M., Stamm, C., Brueggen, J., Jensen, M.R., Schnell, C., Schmid, H., Wartmann, M., Berghausen, J., Drueckes, P., Zimmerlin, A., Bussiere, D., Murray, J., Graus Porta, D., 2011. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamin o]- pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem 54, 7066-7083. • Guagnano, V., Kauffmann, A., Wohrle, S., Stamm, C., Ito, M., Barys, L., Pornon, A., Yao, Y., Li, F., Zhang, Y., Chen, Z., Wilson, C.J., Bordas, V., Le Douget, M., Gaither, L.A., Borawski, J., Monahan, J.E., Venkatesan, K., Brummendorf, T., Thomas, D.M., Garcia-Echeverria, C., Hofmann, F., Sellers, W.R., Graus-Porta, D., 2012. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov 2, 1118-1133. • Gunasekaran, K., Ramakrishnan, C., Balaram, P., 1997. Beta-hairpins in proteins revisited: lessons for de novo design. Protein Eng 10, 1131-1141. • Hagel, M., Miduturu, C., Sheets, M., Rubin, N., Weng, W., Stransky, N., Bifulco, N., Kim, J.L., Hodous, B., Brooijmans, N., Shutes, A., Winter, C., Lengauer, C., Kohl, N.E., Guzi, T., 2015. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of • Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov 5, 424-437.
• Harimoto, N., Taguchi, K., Shirabe, K., Adachi, E., Sakaguchi, Y., Toh, Y., Okamura, T., Kayashima, H., Taketomi, A., Maehara, Y., 2010. The significance of fibroblast growth factor receptor 2 expression in differentiation of hepatocellular carcinoma. Oncology 78, 361-368.
• Helsten, T., Elkin, S., Arthur, E., Tomson, B.N., Carter, J., Kurzrock, R., 2016. The FGFR Landscape in Cancer: Analysis of 4,853 Tumors by Next-Generation Sequencing. Clin Cancer Res 22, 259-267.
• Hierro, C., Alsina, M., Sanchez, M., Serra, V., Rodon, J., Tabernero, J., 2017. Targeting the fibroblast growth factor receptor 2 in gastric cancer: promise or pitfall? Ann Oncol 28, 1207-1216.
• Hierro, C., Rodon, J., Tabernero, J., 2015. Fibroblast Growth Factor (FGF) Receptor/FGF Inhibitors: Novel Targets and Strategies for Optimization of Response of Solid Tumors. Semin Oncol 42, 801-819.
• Homma, S., 1985. Studies on the establishment and some biological characteristics of cultured human liver cancer 56 cell lines; thir growth, functional and morphological characteristics and temperature sensitivities. Jikeikai Med. J. 32, 289-315.
• Hudis, C.A., 2007. Trastuzumab--mechanism of action and use in clinical practice. N Engl J Med 357, 39-51.
• Huh, N., Utakoji, T., 1981. Production of HBs-antigen by two new human hepatoma cell lines and its enhancement by dexamethasone. Gan 72, 178-179.
• Hyeon, J., Ahn, S., Lee, J.J., Song, D.H., Park, C.K., 2013. Expression of fibroblast growth factor 19 is associated with recurrence and poor prognosis of hepatocellular carcinoma. Dig Dis Sci 58, 1916-1922.
• Jeske, Y.W., Ali, S., Byron, S.A., Gao, F., Mannel, R.S., Ghebre, R.G., DiSilvestro, P.A., Lele, S.B., Pearl, M.L., Schmidt, A.P., Lankes, H.A., Ramirez, N.C., Rasty, G., Powell, M., Goodfellow, P.J., Pollock, P.M., 2017. FGFR2 mutations are associated with poor outcomes in endometrioid endometrial cancer: An NRG Oncology/Gynecologic Oncology Group study. Gynecol Oncol 145, 366-373.
• Johnson, D.E., Lu, J., Chen, H., Werner, S., Williams, L.T., 1991. The human fibroblast growth factor receptor genes: a common structural arrangement underlies the mechanisms for generating receptor forms that differ in their third immunoglobulin domain. Mol Cell Biol 11, 4627-4634.
• Kakiuchi, M., Nishizawa, T., Ueda, H., Gotoh, K., Tanaka, A., Hayashi, A., Yamamoto, S., Tatsuno, K., Katoh, H., Watanabe, Y., Ichimura, T., Ushiku, T., Funahashi, S., Tateishi, K., Wada, I., Shimizu, N., Nomura, S., Koike, K., Seto, Y., Fukayama, M., Aburatani, H., Ishikawa, S., 2014. Recurrent gain-of-function mutations of RHOA in diffuse-type gastric carcinoma. Nat Genet 46, 583-587.
• Katoh, M., 2019. Fibroblast growth factor receptors as treatment targets in clinical oncology. Nat Rev Clin Oncol 16, 105-122.
• Kharitonenkov, A., Shiyanova, T.L., Koester, A., Ford, A.M., Micanovic, R., Galbreath, E.J., Sandusky, G.E., Hammond, L.J., Moyers, J.S., Owens, R.A., Gromada, J., Brozinick, J.T., Hawkins, E.D., Wroblewski, V.J., Li, D.S., Mehrbod, F., Jaskunas, S.R., Shanafelt, A.B., 2005. FGF-21 as a novel metabolic regulator. J Clin Invest 115, 1627-1635.
• Kikuchi, A., Suzuki, T., Nakazawa, T., Iizuka, M., Nakayama, A., Ozawa, T., Kameda, M., Shindoh, N., Terasaka, T., Hirano, M., Kuromitsu, S., 2017. ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance. Cancer Sci 108, 236-242.
• Kim, R.D., Sarker, D., Meyer, T., Yau, T., Macarulla, T., Park, J.W., Choo, S.P., Hollebecque, A., Sung, M.W., Lim, H.Y., Mazzaferro, V., Trojan, J., Zhu, A.X., Yoon, J.H., Sharma, S., Lin, Z.Z., Chan, S.L., Faivre, S., Feun, L.G., Yen, C.J., Dufour, J.F., Palmer, D.H., Llovet, J.M., Manoogian, M., Tugnait, M., Stransky, N., Hagel, M., Kohl, N.E., Lengauer, C., Sherwin, C.A., Schmidt-Kittler, O., Hoeflich, K.P., Shi, H., Wolf, B.B., Kang, Y.K., 2019. First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant FGF19 Signaling as a Driver Event in Hepatocellular Carcinoma. Cancer Discov 9, 1696-1707.
• Kong, K., Ng, P.K., Scott, K.L., 2017. Ba/F3 transformation assays, Oncotarget, United States, pp. 35488-35489.
• Lang, L., Shull, A.Y., Teng, Y., 2019. Interrupting the FGF19-FGFR4 Axis to Therapeutically Disrupt Cancer Progression. Curr Cancer Drug Targets 19, 17-25.
• Lee, Y.T., Tan, Y.J., Oon, C.E., 2018. Molecular targeted therapy: Treating cancer with specificity. Eur J Pharmacol 834, 188-196.
• Lesca, E., Lammens, A., Huber, R., Augustin, M., 2014. Structural analysis of the human fibroblast growth factor receptor 4 kinase. J Mol Biol 426, 3744-3756.
• Liang, G., Chen, G., Wei, X., Zhao, Y., Li, X., 2013. Small molecule inhibition of fibroblast growth factor receptors in cancer. Cytokine Growth Factor Rev 24, 467-475.
• Lin, B.C., Desnoyers, L.R., 2012. FGF19 and cancer. Adv Exp Med Biol 728, 183-194.
• Liu, X., Meltzer, S.J., 2017. Gastric Cancer in the Era of Precision Medicine. Cell Mol Gastroenterol Hepatol 3, 348-358.
• Lott, S., Wang, M., Zhang, S., MacLennan, G.T., Lopez-Beltran, A., Montironi, R., Sung, M.T., Tan, P.H., Cheng, L., 2009. FGFR3 and TP53 mutation analysis in inverted urothelial papilloma: incidence and etiological considerations. Mod Pathol 22, 627-632.
• Luo, J., Liu, S., Leung, S., Gru, A.A., Tao, Y., Hoog, J., Ho, J., Davies, S.R., Allred, D.C., Salavaggione, A.L., Snider, J., Mardis, E.R., Nielsen, T.O., Ellis, M.J., 2017. An mRNA Gene Expression-Based Signature to Identify FGFR1-Amplified Estrogen Receptor-Positive Breast Tumors. J Mol Diagn 19, 147-161.
• Malik, S.M., Maher, V.E., Bijwaard, K.E., Becker, R.L., Zhang, L., Tang, S.W., Song, P., Liu, Q., Marathe, A., Gehrke, B., Helms, W., Hanner, D., Justice, R., Pazdur, R., 2014. U.S. Food and Drug Administration approval: crizotinib for treatment of advanced or metastatic non-small cell lung cancer that is anaplastic lymphoma kinase positive. Clin Cancer Res 20, 2029-2034.
• Mariotto, A.B., Yabroff, K.R., Shao, Y., Feuer, E.J., Brown, M.L., 2011. Projections of the cost of cancer care in the United States: 2010-2020. J Natl Cancer Inst 103, 117-128.
• Milner-White, E.J., Poet, R., 1986. Four classes of beta-hairpins in proteins. Biochem J 240, 289-292.
• Miura, S., Mitsuhashi, N., Shimizu, H., Kimura, F., Yoshidome, H., Otsuka, M., Kato, A., Shida, T., Okamura, D., Miyazaki, M., 2012. Fibroblast growth factor 19 expression correlates with tumor progression and poorer prognosis of hepatocellular carcinoma. BMC Cancer 12, 56.
• Morimoto, Y., Ozaki, T., Ouchida, M., Umehara, N., Ohata, N., Yoshida, A., Shimizu, K., Inoue, H., 2003. Single nucleotide polymorphism in fibroblast growth factor receptor 4 at codon 388 is associated with prognosis in highgrade soft tissue sarcoma. Cancer 98, 2245-2250.
• Murray, C.J., Vos, T., Lozano, R., Naghavi, M., Flaxman, A.D., Michaud, C., Ezzati, M., Shibuya, K., Salomon, J.A., Abdalla, S., Aboyans, V., Abraham, J., Ackerman, I., Aggarwal, R., Ahn, S.Y., Ali, M.K., Alvarado, M., Anderson, H.R., Anderson, L.M., Andrews, K.G., Atkinson, C., Baddour, L.M., Bahalim, A.N., Barker-Collo, S., Barrero, L.H., Bartels, D.H., Basanez, M.G., Baxter, A., Bell, M.L., Benjamin, E.J., Bennett, D., Bernabe, E., Bhalla, K., Bhandari, B., Bikbov, B., Bin Abdulhak, A., Birbeck, G., Black, J.A., Blencowe, H., Blore, J.D., Blyth, F., Bolliger, I., Bonaventure, A., Boufous, S., Bourne, R., Boussinesq, M., Braithwaite, T., Brayne, C., Bridgett, L., Brooker, S., Brooks, P., Brugha, T.S., Bryan-Hancock, C., Bucello, C., Buchbinder, R., Buckle, G., Budke, C.M., Burch, M., Burney, P., Burstein, R., Calabria, B., Campbell, B., Canter, C.E., Carabin, H., Carapetis, J., Carmona, L., Cella, C., Charlson, F., Chen, H., Cheng, A.T., Chou, D., Chugh, S.S., Coffeng, L.E., Colan, S.D., Colquhoun, S., Colson, K.E., Condon, J., Connor, M.D., Cooper, L.T., Corriere, M., Cortinovis, M., de Vaccaro, K.C., Couser, W., Cowie, B.C., Criqui, M.H., Cross, M., Dabhadkar, K.C., Dahiya, M., Dahodwala, N., DamsereDerry, J., Danaei, G., Davis, A., De Leo, D., Degenhardt, L., Dellavalle, R., Delossantos, A., Denenberg, J., Derrett, S., Des Jarlais, D.C., Dharmaratne, S.D., Dherani, M., Diaz-Torne, C., Dolk, H., Dorsey, E.R., Driscoll, T., Duber, H., Ebel, B., Edmond, K., Elbaz, A., Ali, S.E., Erskine, H., Erwin, P.J., Espindola, P., Ewoigbokhan, S.E., Farzadfar, F., Feigin, V., Felson, D.T., Ferrari, A., Ferri, C.P., Fevre, E.M., Finucane, M.M., Flaxman, S., Flood, L., Foreman, K., Forouzanfar, M.H., Fowkes, F.G., Fransen, M., Freeman, M.K., Gabbe, B.J., Gabriel, 58 S.E., Gakidou, E., Ganatra, H.A., Garcia, B., Gaspari, F., Gillum, R.F., Gmel, G., Gonzalez-Medina, D., Gosselin, R., Grainger, R., Grant, B., Groeger, J., Guillemin, F., Gunnell, D., Gupta, R., Haagsma, J., Hagan, H., Halasa, Y.A., Hall, W., Haring, D., Haro, J.M., Harrison, J.E., Havmoeller, R., Hay, R.J., Higashi, H., Hill, C., Hoen, B., Hoffman, H., Hotez, P.J., Hoy, D., Huang, J.J., Ibeanusi, S.E., Jacobsen, K.H., James, S.L., Jarvis, D., Jasrasaria, R., Jayaraman, S., Johns, N., Jonas, J.B., Karthikeyan, G., Kassebaum, N., Kawakami, N., Keren, A., Khoo, J.P., King, C.H., Knowlton, L.M., Kobusingye, O., Koranteng, A., Krishnamurthi, R., Laden, F., Lalloo, R., Laslett, L.L., Lathlean, T., Leasher, J.L., Lee, Y.Y., Leigh, J., Levinson, D., Lim, S.S., Limb, E., Lin, J.K., Lipnick, M., Lipshultz, S.E., Liu, W., Loane, M., Ohno, S.L., Lyons, R., Mabweijano, J., MacIntyre, M.F., Malekzadeh, R., Mallinger, L., Manivannan, S., Marcenes, W., March, L., Margolis, D.J., Marks, G.B., Marks, R., Matsumori, A., Matzopoulos, R., Mayosi, B.M., McAnulty, J.H., McDermott, M.M., McGill, N., McGrath, J., Medina-Mora, M.E., Meltzer, M., Mensah, G.A., Merriman, T.R., Meyer, A.C., Miglioli, V., Miller, M., Miller, T.R., Mitchell, P.B., Mock, C., Mocumbi, A.O., Moffitt, T.E., Mokdad, A.A., Monasta, L., Montico, M., Moradi-Lakeh, M., Moran, A., Morawska, L., Mori, R., Murdoch, M.E., Mwaniki, M.K., Naidoo, K., Nair, M.N., Naldi, L., Narayan, K.M., Nelson, P.K., Nelson, R.G., Nevitt, M.C., Newton, C.R., Nolte, S., Norman, P., Norman, R., O'Donnell, M., O'Hanlon, S., Olives, C., Omer, S.B., Ortblad, K., Osborne, R., Ozgediz, D., Page, A., Pahari, B., Pandian, J.D., Rivero, A.P., Patten, S.B., Pearce, N., Padilla, R.P., Perez-Ruiz, F., Perico, N., Pesudovs, K., Phillips, D., Phillips, M.R., Pierce, K., Pion, S., Polanczyk, G.V., Polinder, S., Pope, C.A., 3rd, Popova, S., Porrini, E., Pourmalek, F., Prince, M., Pullan, R.L., Ramaiah, K.D., Ranganathan, D., Razavi, H., Regan, M., Rehm, J.T., Rein, D.B., Remuzzi, G., Richardson, K., Rivara, F.P., Roberts, T., Robinson, C., De Leon, F.R., Ronfani, L., Room, R., Rosenfeld, L.C., Rushton, L., Sacco, R.L., Saha, S., Sampson, U., Sanchez-Riera, L., Sanman, E., Schwebel, D.C., Scott, J.G., Segui-Gomez, M., Shahraz, S., Shepard, D.S., Shin, H., Shivakoti, R., Singh, D., Singh, G.M., Singh, J.A., Singleton, J., Sleet, D.A., Sliwa, K., Smith, E., Smith, J.L., Stapelberg, N.J., Steer, A., Steiner, T., Stolk, W.A., Stovner, L.J., Sudfeld, C., Syed, S., Tamburlini, G., Tavakkoli, M., Taylor, H.R., Taylor, J.A., Taylor, W.J., Thomas, B., Thomson, W.M., Thurston, G.D., Tleyjeh, I.M., Tonelli, M., Towbin, J.A., Truelsen, T., Tsilimbaris, M.K., Ubeda, C., Undurraga, E.A., van der Werf, M.J., van Os, J., Vavilala, M.S., Venketasubramanian, N., Wang, M., Wang, W., Watt, K., Weatherall, D.J., Weinstock, M.A., Weintraub, R., Weisskopf, M.G., Weissman, M.M., White, R.A., Whiteford, H., Wiebe, N., Wiersma, S.T., Wilkinson, J.D., Williams, H.C., Williams, S.R., Witt, E., Wolfe, F., Woolf, A.D., Wulf, S., Yeh, P.H., Zaidi, A.K., Zheng, Z.J., Zonies, D., Lopez, A.D., AlMazroa, M.A., Memish, Z.A., 2012. Disability-adjusted life years (DALYs) for 291 diseases and injuries in 21 regions, 1990-2010: a systematic analysis for the Global Burden of Disease Study 2010. Lancet 380, 2197-2223.
• Nakabayashi, H., Taketa, K., Miyano, K., Yamane, T., Sato, J., 1982. Growth of human hepatoma cells lines with differentiated functions in chemically defined medium. Cancer Res 42, 3858-3863.
• Nicholes, K., Guillet, S., Tomlinson, E., Hillan, K., Wright, B., Frantz, G.D., Pham, T.A., Dillard-Telm, L., Tsai, S.P., Stephan, J.P., Stinson, J., Stewart, T., French, D.M., 2002. A mouse model of hepatocellular carcinoma: ectopic expression of fibroblast growth factor 19 in skeletal muscle of transgenic mice. Am J Pathol 160, 2295- 2307.
• Nyeng, P., Norgaard, G.A., Kobberup, S., Jensen, J., 2007. FGF10 signaling controls stomach morphogenesis. Dev Biol 303, 295-310.
• Ornitz, D.M., Itoh, N., 2015. The Fibroblast Growth Factor signaling pathway. Wiley Interdiscip Rev Dev Biol 4, 215-266. 59
• Pao, W., Miller, V., Zakowski, M., Doherty, J., Politi, K., Sarkaria, I., Singh, B., Heelan, R., Rusch, V., Fulton, L., Mardis, E., Kupfer, D., Wilson, R., Kris, M., Varmus, H., 2004. EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A 101, 13306-13311.
• Park, J.G., Lee, J.H., Kang, M.S., Park, K.J., Jeon, Y.M., Lee, H.J., Kwon, H.S., Park, H.S., Yeo, K.S., Lee, K.U., et al., 1995. Characterization of cell lines established from human hepatocellular carcinoma. Int J Cancer 62, 276- 282.
• Patani, H., Bunney, T.D., Thiyagarajan, N., Norman, R.A., Ogg, D., Breed, J., Ashford, P., Potterton, A., Edwards, M., Williams, S.V., Thomson, G.S., Pang, C.S., Knowles, M.A., Breeze, A.L., Orengo, C., Phillips, C., Katan, M., 2016. Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use. Oncotarget 7, 24252-24268.
• Paur, J., Nika, L., Maier, C., Moscu-Gregor, A., Kostka, J., Huber, D., Mohr, T., Heffeter, P., Schrottmaier, W.C., Kappel, S., Kandioler, D., Holzmann, K., Marian, B., Berger, W., Grusch, M., Grasl-Kraupp, B., 2015. Fibroblast growth factor receptor 3 isoforms: Novel therapeutic targets for hepatocellular carcinoma? Hepatology 62, 1767- 1778.
• Peifer, M., Fernandez-Cuesta, L., Sos, M.L., George, J., Seidel, D., Kasper, L.H., Plenker, D., Leenders, F., Sun, R., Zander, T., Menon, R., Koker, M., Dahmen, I., Muller, C., Di Cerbo, V., Schildhaus, H.U., Altmuller, J., Baessmann, I., Becker, C., de Wilde, B., Vandesompele, J., Bohm, D., Ansen, S., Gabler, F., Wilkening, I., Heynck, S., Heuckmann, J.M., Lu, X., Carter, S.L., Cibulskis, K., Banerji, S., Getz, G., Park, K.S., Rauh, D., Grutter, C., Fischer, M., Pasqualucci, L., Wright, G., Wainer, Z., Russell, P., Petersen, I., Chen, Y., Stoelben, E., Ludwig, C., Schnabel, P., Hoffmann, H., Muley, T., Brockmann, M., Engel-Riedel, W., Muscarella, L.A., Fazio, V.M., Groen, H., Timens, W., Sietsma, H., Thunnissen, E., Smit, E., Heideman, D.A., Snijders, P.J., Cappuzzo, F., Ligorio, C., Damiani, S., Field, J., Solberg, S., Brustugun, O.T., Lund-Iversen, M., Sanger, J., Clement, J.H., Soltermann, A., Moch, H., Weder, W., Solomon, B., Soria, J.C., Validire, P., Besse, B., Brambilla, E., Brambilla, C., Lantuejoul, S., Lorimier, P., Schneider, P.M., Hallek, M., Pao, W., Meyerson, M., Sage, J., Shendure, J., Schneider, R., Buttner, R., Wolf, J., Nurnberg, P., Perner, S., Heukamp, L.C., Brindle, P.K., Haas, S., Thomas, R.K., 2012. Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer. Nat Genet 44, 1104-1110.
• Perera, T.P.S., Jovcheva, E., Mevellec, L., Vialard, J., De Lange, D., Verhulst, T., Paulussen, C., Van De Ven, K., King, P., Freyne, E., Rees, D.C., Squires, M., Saxty, G., Page, M., Murray, C.W., Gilissen, R., Ward, G., Thompson, N.T., Newell, D.R., Cheng, N., Xie, L., Yang, J., Platero, S.J., Karkera, J.D., Moy, C., Angibaud, P., Laquerre, S., Lorenzi, M.V., 2017. Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor. Mol Cancer Ther 16, 1010-1020.
• Poon, R.T., 2011. Prevention of recurrence after resection of hepatocellular carcinoma: a daunting challenge. Hepatology 54, 757-759.
• Qiu, W.H., Zhou, B.S., Chu, P.G., Chen, W.G., Chung, C., Shih, J., Hwu, P., Yeh, C., Lopez, R., Yen, Y., 2005. Over-expression of fibroblast growth factor receptor 3 in human hepatocellular carcinoma. World J Gastroenterol 11, 5266-5272.
• Razzaque, M.S., Lanske, B., 2007. The emerging role of the fibroblast growth factor-23-klotho axis in renal regulation of phosphate homeostasis. J Endocrinol 194, 1-10.
• Roidl, A., Foo, P., Wong, W., Mann, C., Bechtold, S., Berger, H.J., Streit, S., Ruhe, J.E., Hart, S., Ullrich, A., Ho, H.K., 2010. The FGFR4 Y367C mutant is a dominant oncogene in MDA-MB453 breast cancer cells. Oncogene 29, 1543-1552.
• Romond, E.H., Perez, E.A., Bryant, J., Suman, V.J., Geyer, C.E., Jr., Davidson, N.E., Tan-Chiu, E., Martino, S., Paik, S., Kaufman, P.A., Swain, S.M., Pisansky, T.M., Fehrenbacher, L., Kutteh, L.A., Vogel, V.G., Visscher, D.W., Yothers, G., Jenkins, R.B., Brown, A.M., Dakhil, S.R., Mamounas, E.P., Lingle, W.L., Klein, P.M., Ingle, J.N., Wolmark, N., 2005. Trastuzumab plus adjuvant chemotherapy for operable HER2-positive breast cancer. N Engl J Med 353, 1673-1684.
• Sandhu, D.S., Baichoo, E., Roberts, L.R., 2014. Fibroblast growth factor signaling in liver carcinogenesis. Hepatology 59, 1166-1173.
• Sawey, E.T., Chanrion, M., Cai, C., Wu, G., Zhang, J., Zender, L., Zhao, A., Busuttil, R.W., Yee, H., Stein, L., French, D.M., Finn, R.S., Lowe, S.W., Powers, S., 2011. Identification of a therapeutic strategy targeting amplified FGF19 in liver cancer by Oncogenomic screening. Cancer Cell 19, 347-358.
• Spangenberg, H.C., Thimme, R., Blum, H.E., 2009. Targeted therapy for hepatocellular carcinoma. Nat Rev Gastroenterol Hepatol 6, 423-432.
• Strumberg, D., Richly, H., Hilger, R.A., Schleucher, N., Korfee, S., Tewes, M., Faghih, M., Brendel, E., Voliotis, D., Haase, C.G., Schwartz, B., Awada, A., Voigtmann, R., Scheulen, M.E., Seeber, S., 2005. Phase I clinical and pharmacokinetic study of the Novel Raf kinase and vascular endothelial growth factor receptor inhibitor BAY 43- 9006 in patients with advanced refractory solid tumors. J Clin Oncol 23, 965-972.
• Tanner, Y., Grose, R.P., 2016. Dysregulated FGF signalling in neoplastic disorders. Semin Cell Dev Biol 53, 126- 135.
• Taylor, J.G.t., Cheuk, A.T., Tsang, P.S., Chung, J.Y., Song, Y.K., Desai, K., Yu, Y., Chen, Q.R., Shah, K., Youngblood, V., Fang, J., Kim, S.Y., Yeung, C., Helman, L.J., Mendoza, A., Ngo, V., Staudt, L.M., Wei, J.S., Khanna, C., Catchpoole, D., Qualman, S.J., Hewitt, S.M., Merlino, G., Chanock, S.J., Khan, J., 2009. Identification of FGFR4-activating mutations in human rhabdomyosarcomas that promote metastasis in xenotransplanted models. J Clin Invest 119, 3395-3407.
• Tchaicha, J.H., Akbay, E.A., Altabef, A., Mikse, O.R., Kikuchi, E., Rhee, K., Liao, R.G., Bronson, R.T., Sholl, L.M., Meyerson, M., Hammerman, P.S., Wong, K.K., 2014. Kinase domain activation of FGFR2 yields highgrade lung adenocarcinoma sensitive to a Pan-FGFR inhibitor in a mouse model of NSCLC. Cancer Res 74, 4676- 4684.
• Tomlinson, E., Fu, L., John, L., Hultgren, B., Huang, X., Renz, M., Stephan, J.P., Tsai, S.P., Powell-Braxton, L., French, D., Stewart, T.A., 2002. Transgenic mice expressing human fibroblast growth factor-19 display increased metabolic rate and decreased adiposity. Endocrinology 143, 1741-1747.
• Turner, N., Grose, R., 2010. Fibroblast growth factor signalling: from development to cancer. Nat Rev Cancer 10, 116-129.
• Turner, N., Lambros, M.B., Horlings, H.M., Pearson, A., Sharpe, R., Natrajan, R., Geyer, F.C., van Kouwenhove, M., Kreike, B., Mackay, A., Ashworth, A., van de Vijver, M.J., Reis-Filho, J.S., 2010. Integrative molecular profiling of triple negative breast cancers identifies amplicon drivers and potential therapeutic targets. Oncogene 29, 2013-2023.
• Verstraete, M., Debucquoy, A., Gonnissen, A., Dok, R., Isebaert, S., Devos, E., McBride, W., Haustermans, K., 2015. In vitro and in vivo evaluation of the radiosensitizing effect of a selective FGFR inhibitor (JNJ-42756493) for rectal cancer. BMC Cancer 15, 946.
• Wang, J., Yu, W., Cai, Y., Ren, C., Ittmann, M.M., 2008. Altered fibroblast growth factor receptor 4 stability promotes prostate cancer progression. Neoplasia 10, 847-856.
• Weiss, J., Sos, M.L., Seidel, D., Peifer, M., Zander, T., Heuckmann, J.M., Ullrich, R.T., Menon, R., Maier, S., Soltermann, A., Moch, H., Wagener, P., Fischer, F., Heynck, S., Koker, M., Schottle, J., Leenders, F., Gabler, F., Dabow, I., Querings, S., Heukamp, L.C., Balke-Want, H., Ansen, S., Rauh, D., Baessmann, I., Altmuller, J., Wainer, Z., Conron, M., Wright, G., Russell, P., Solomon, B., Brambilla, E., Brambilla, C., Lorimier, P., Sollberg, S., Brustugun, O.T., Engel-Riedel, W., Ludwig, C., Petersen, I., Sanger, J., Clement, J., Groen, H., Timens, W., Sietsma, H., Thunnissen, E., Smit, E., Heideman, D., Cappuzzo, F., Ligorio, C., Damiani, S., Hallek, M., Beroukhim, R., Pao, W., Klebl, B., Baumann, M., Buettner, R., Ernestus, K., Stoelben, E., Wolf, J., Nurnberg, P., Perner, S., Thomas, R.K., 2010. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer. Sci Transl Med 2, 62ra93.
• Wu, Y.M., Su, F., Kalyana-Sundaram, S., Khazanov, N., Ateeq, B., Cao, X., Lonigro, R.J., Vats, P., Wang, R., Lin, S.F., Cheng, A.J., Kunju, L.P., Siddiqui, J., Tomlins, S.A., Wyngaard, P., Sadis, S., Roychowdhury, S., Hussain, M.H., Feng, F.Y., Zalupski, M.M., Talpaz, M., Pienta, K.J., Rhodes, D.R., Robinson, D.R., Chinnaiyan, A.M., 2013. Identification of targetable FGFR gene fusions in diverse cancers. Cancer Discov 3, 636-647.
• Yamamoto, N., Ryoo, B.Y., Keam, B., Kudo, M., Lin, C.C., Kunieda, F., Ball, H.A., Moran, D., Komatsu, K., Takeda, K., Fukuda, M., Furuse, J., Morita, S., Doi, T., 2019. A phase 1 study of oral ASP5878, a selective smallmolecule inhibitor of fibroblast growth factor receptors 1-4, as a single dose and multiple doses in patients with solid malignancies. Invest New Drugs.
• Yang, C., Lu, W., Lin, T., You, P., Ye, M., Huang, Y., Jiang, X., Wang, C., Wang, F., Lee, M.H., Yeung, S.C., Johnson, R.L., Wei, C., Tsai, R.Y., Frazier, M.L., McKeehan, W.L., Luo, Y., 2013. Activation of Liver FGF21 in hepatocarcinogenesis and during hepatic stress. BMC Gastroenterol 13, 67.
• Ye, Y., Shi, Y., Zhou, Y., Du, C., Wang, C., Zhan, H., Zheng, B., Cao, X., Sun, M.H., Fu, H., 2010. The fibroblast growth factor receptor-4 Arg388 allele is associated with gastric cancer progression. Ann Surg Oncol 17, 3354- 3361.
論文の公開元へ
