메뉴 건너뛰기




Volumn 5, Issue 4, 2015, Pages 424-437

First selective small molecule inhibitor of FGFR4 for the treatment of hepatocellular carcinomas with an activated FGFR4 signaling pathway

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; CASPASE 3; CASPASE 7; FIBROBLAST GROWTH FACTOR 19; FIBROBLAST GROWTH FACTOR RECEPTOR 4; KI 67 ANTIGEN; KLOTHO PROTEIN; MESSENGER RNA; N (2 ((6 (2,6 DICHLORO 3,5 DIMETHOXYPHENYL)QUINAZOLIN 2 YL)AMINO) 3 METHYLPHENYL)ACRYLAMIDE; SORAFENIB; UNCLASSIFIED DRUG; PROTEIN BINDING; PROTEIN KINASE INHIBITOR;

EID: 84939482520     PISSN: 21598274     EISSN: 21598290     Source Type: Journal    
DOI: 10.1158/2159-8290.CD-14-1029     Document Type: Article
Times cited : (244)

References (35)
  • 3
    • 57749189578 scopus 로고    scopus 로고
    • Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: A phase III randomised, doubleblind, placebo-controlled trial
    • Cheng A-L, Kang Y-K, Chen Z, Tsao C-J, Qin S, Kim JS, et al. Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, doubleblind, placebo-controlled trial. Lancet Oncol 2009; 10: 25-34.
    • (2009) Lancet Oncol , vol.10 , pp. 25-34
    • Cheng, A.-L.1    Kang, Y.-K.2    Chen, Z.3    Tsao, C.-J.4    Qin, S.5    Kim, J.S.6
  • 4
    • 84859393351 scopus 로고    scopus 로고
    • Integrative genomic identification of genes on 8p associated with hepatocellular carcinoma progression and patient survival
    • Roessler S, Long EL, Budhu A, Chen Y, Zhao X, Ji J, et al. Integrative genomic identification of genes on 8p associated with hepatocellular carcinoma progression and patient survival. Gastroenterology 2012; 142: 957-66. e12.
    • (2012) Gastroenterology , vol.142 , pp. 957
    • Roessler, S.1    Long, E.L.2    Budhu, A.3    Chen, Y.4    Zhao, X.5    Ji, J.6
  • 5
    • 53049086329 scopus 로고    scopus 로고
    • Focal gains of VEGFA and molecular classification of hepatocellular carcinoma
    • Chiang DY, Villanueva A, Hoshida Y, Peix J, Newell P, Minguez B, et al. Focal gains of VEGFA and molecular classification of hepatocellular carcinoma. Cancer Res 2008; 68: 6779-88.
    • (2008) Cancer Res , vol.68 , pp. 6779-6788
    • Chiang, D.Y.1    Villanueva, A.2    Hoshida, Y.3    Peix, J.4    Newell, P.5    Minguez, B.6
  • 6
    • 79952497178 scopus 로고    scopus 로고
    • Identification of a therapeutic strategy targeting amplified FGF19 in liver cancer by oncogenomic screening
    • Sawey ET, Chanrion M, Cai C, Wu G, Zhang J, Zender L, et al. Identification of a therapeutic strategy targeting amplified FGF19 in liver cancer by oncogenomic screening. Cancer Cell 2011; 19: 347- 58.
    • (2011) Cancer Cell , vol.19 , pp. 347-358
    • Sawey, E.T.1    Chanrion, M.2    Cai, C.3    Wu, G.4    Zhang, J.5    Zender, L.6
  • 7
    • 84861625981 scopus 로고    scopus 로고
    • Integrated analysis of somatic mutations and focal copynumber changes identifies key genes and pathways in hepatocellular carcinoma
    • Guichard C, Amaddeo G, Imbeaud S, Ladeiro Y, Pelletier L, Maad IB, et al. Integrated analysis of somatic mutations and focal copynumber changes identifies key genes and pathways in hepatocellular carcinoma. Nat Genet 2012; 44: 694-8.
    • (2012) Nat Genet , vol.44 , pp. 694-698
    • Guichard, C.1    Amaddeo, G.2    Imbeaud, S.3    Ladeiro, Y.4    Pelletier, L.5    Maad, I.B.6
  • 8
    • 84901472677 scopus 로고    scopus 로고
    • Genomic portrait of resectable hepatocellular carcinomas: Implications of RB1 and FGF19 aberrations for patient stratification
    • Ahn S-M, Jang SJ, Shim JH, Kim D, Hong S-M, Sung CO, et al. Genomic portrait of resectable hepatocellular carcinomas: implications of RB1 and FGF19 aberrations for patient stratification. Hepatology 2014; 60: 1972-82.
    • (2014) Hepatology , vol.60 , pp. 1972-1982
    • Ahn, S.-M.1    Jang, S.J.2    Shim, J.H.3    Kim, D.4    Hong, S.-M.5    Sung, C.O.6
  • 11
    • 79952803104 scopus 로고    scopus 로고
    • FGF19 regulates cell proliferation, glucose and bile acid metabolism via FGFR4-dependent and independent pathways
    • Wu A-L, Coulter S, Liddle C, Wong A, Eastham-Anderson J, French DM, et al. FGF19 regulates cell proliferation, glucose and bile acid metabolism via FGFR4-dependent and independent pathways. PLoS One 2011; 6: e17868.
    • (2011) PLoS One , vol.6
    • Wu, A.-L.1    Coulter, S.2    Liddle, C.3    Wong, A.4    Eastham-Anderson, J.5    French, D.M.6
  • 12
    • 37849029159 scopus 로고    scopus 로고
    • Targeting FGF19 inhibits tumor growth in colon cancer xenograft and FGF19 transgenic hepatocellular carcinoma models
    • Desnoyers LR, Pai R, Ferrando RE, Hotzel K, Le T, Ross J, et al. Targeting FGF19 inhibits tumor growth in colon cancer xenograft and FGF19 transgenic hepatocellular carcinoma models. Oncogene 2008; 27: 85-97.
    • (2008) Oncogene , vol.27 , pp. 85-97
    • Desnoyers, L.R.1    Pai, R.2    Ferrando, R.E.3    Hotzel, K.4    Le, T.5    Ross, J.6
  • 13
    • 84866171951 scopus 로고    scopus 로고
    • Targeting FGFR4 inhibits hepatocellular carcinoma in preclinical mouse models
    • French DM, Lin BC, Wang M, Adams C, Shek T, Hotzel K, et al. Targeting FGFR4 inhibits hepatocellular carcinoma in preclinical mouse models. PloS One 2012; 7: e36713.
    • (2012) PloS One , vol.7
    • French, D.M.1    Lin, B.C.2    Wang, M.3    Adams, C.4    Shek, T.5    Hotzel, K.6
  • 14
    • 81055124246 scopus 로고    scopus 로고
    • A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models
    • Zhao G, Li W-Y, Chen D, Henry JR, Li H-Y, Chen Z, et al. A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. Mol Cancer Ther 2011; 10: 2200-10.
    • (2011) Mol Cancer Ther , vol.10 , pp. 2200-2210
    • Zhao, G.1    Li, W.-Y.2    Chen, D.3    Henry, J.R.4    Li, H.-Y.5    Chen, Z.6
  • 15
    • 84859402751 scopus 로고    scopus 로고
    • Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models
    • Gozgit JM, Wong MJ, Moran L, Wardwell S, Mohemmad QK, Narasimhan NI, et al. Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models. Mol Cancer Ther 2012; 11: 690-9.
    • (2012) Mol Cancer Ther , vol.11 , pp. 690-699
    • Gozgit, J.M.1    Wong, M.J.2    Moran, L.3    Wardwell, S.4    Mohemmad, Q.K.5    Narasimhan, N.I.6
  • 16
    • 80054900437 scopus 로고    scopus 로고
    • Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4- (4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase
    • Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, et al. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4- (4-ethyl-piperazin-1-yl)-phenylamino]-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 2011; 54: 7066-83.
    • (2011) J Med Chem , vol.54 , pp. 7066-7083
    • Guagnano, V.1    Furet, P.2    Spanka, C.3    Bordas, V.4    Le Douget, M.5    Stamm, C.6
  • 17
    • 84860120185 scopus 로고    scopus 로고
    • AZD4547: An orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family
    • Gavine PR, Mooney L, Kilgour E, Thomas AP, Al-Kadhimi K, Beck S, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res 2012; 72: 2045-56.
    • (2012) Cancer Res , vol.72 , pp. 2045-2056
    • Gavine, P.R.1    Mooney, L.2    Kilgour, E.3    Thomas, A.P.4    Al-Kadhimi, K.5    Beck, S.6
  • 18
    • 84876048479 scopus 로고    scopus 로고
    • Fibroblast growth factor receptor inhibitors as a cancer treatment: From a biologic rationale to medical perspectives
    • Dieci MV, Arnedos M, Andre F, Soria JC. Fibroblast growth factor receptor inhibitors as a cancer treatment: from a biologic rationale to medical perspectives. Cancer Discov 2013; 3: 264-79.
    • (2013) Cancer Discov , vol.3 , pp. 264-279
    • Dieci, M.V.1    Arnedos, M.2    Andre, F.3    Soria, J.C.4
  • 19
    • 84874301754 scopus 로고    scopus 로고
    • Developing irreversible inhibitors of the protein kinase cysteinome
    • Liu Q, Sabnis Y, Zhao Z, Zhang T, Buhrlage SJ, Jones LH, et al. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol 2013; 20: 146-59.
    • (2013) Chem Biol , vol.20 , pp. 146-159
    • Liu, Q.1    Sabnis, Y.2    Zhao, Z.3    Zhang, T.4    Buhrlage, S.J.5    Jones, L.H.6
  • 21
    • 77949558462 scopus 로고    scopus 로고
    • A structure-guided approach to creating covalent FGFR inhibitors
    • Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, et al. A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol 2010; 17: 285-95.
    • (2010) Chem Biol , vol.17 , pp. 285-295
    • Zhou, W.1    Hur, W.2    McDermott, U.3    Dutt, A.4    Xian, W.5    Ficarro, S.B.6
  • 22
    • 22244491050 scopus 로고    scopus 로고
    • Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin- 2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases
    • Thompson AM, Delaney AM, Hamby JM, Schroeder MC, Spoon TA, Crean SM, et al. Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin- 2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. J Med Chem 2005; 48: 4628-53.
    • (2005) J Med Chem , vol.48 , pp. 4628-4653
    • Thompson, A.M.1    Delaney, A.M.2    Hamby, J.M.3    Schroeder, M.C.4    Spoon, T.A.5    Crean, S.M.6
  • 23
    • 0032531929 scopus 로고    scopus 로고
    • Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain
    • Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J 1998; 17: 5896-904.
    • (1998) EMBO J , vol.17 , pp. 5896-5904
    • Mohammadi, M.1    Froum, S.2    Hamby, J.M.3    Schroeder, M.C.4    Panek, R.L.5    Lu, G.H.6
  • 25
    • 77949423592 scopus 로고    scopus 로고
    • The FGFR4 Y367C mutant is a dominant oncogene in MDA-MB453 breast cancer cells
    • Roidl A, Foo P, Wong W, Mann C, Bechtold S, Berger HJ, et al. The FGFR4 Y367C mutant is a dominant oncogene in MDA-MB453 breast cancer cells. Oncogene 2010; 29: 1543-52.
    • (2010) Oncogene , vol.29 , pp. 1543-1552
    • Roidl, A.1    Foo, P.2    Wong, W.3    Mann, C.4    Bechtold, S.5    Berger, H.J.6
  • 26
    • 78650451788 scopus 로고    scopus 로고
    • Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer
    • Weiss J, Sos ML, Seidel D, Peifer M, Zander T, Heuckmann JM, et al. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer. Sci Transl Med 2010; 2: 62ra93.
    • (2010) Sci Transl Med , vol.2
    • Weiss, J.1    Sos, M.L.2    Seidel, D.3    Peifer, M.4    Zander, T.5    Heuckmann, J.M.6
  • 27
    • 84871491773 scopus 로고    scopus 로고
    • FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor
    • Guagnano V, Kauffmann A, Wohrle S, Stamm C, Ito M, Barys L, et al. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov 2012; 2: 1118-33.
    • (2012) Cancer Discov , vol.2 , pp. 1118-1133
    • Guagnano, V.1    Kauffmann, A.2    Wohrle, S.3    Stamm, C.4    Ito, M.5    Barys, L.6
  • 28
    • 84859169877 scopus 로고    scopus 로고
    • The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity
    • Barretina J, Caponigro G, Stransky N, Venkatesan K, Margolin AA, Kim S, et al. The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity. Nature 2012; 483: 603-7.
    • (2012) Nature , vol.483 , pp. 603-607
    • Barretina, J.1    Caponigro, G.2    Stransky, N.3    Venkatesan, K.4    Margolin, A.A.5    Kim, S.6
  • 29
    • 78650513897 scopus 로고    scopus 로고
    • Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine
    • Hagel M, Niu D, St Martin T, Sheets MP, Qiao L, Bernard H, et al. Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine. Nat Chem Biol 2011; 7: 22-4.
    • (2011) Nat Chem Biol , vol.7 , pp. 22-24
    • Hagel, M.1    Niu, D.2    St Martin, T.3    Sheets, M.P.4    Qiao, L.5    Bernard, H.6
  • 30
    • 84880447005 scopus 로고    scopus 로고
    • Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans
    • Evans EK, Tester R, Aslanian S, Karp R, Sheets M, Labenski MT, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther 2013; 346: 219-28.
    • (2013) J Pharmacol Exp Ther , vol.346 , pp. 219-228
    • Evans, E.K.1    Tester, R.2    Aslanian, S.3    Karp, R.4    Sheets, M.5    Labenski, M.T.6
  • 31
    • 84897454901 scopus 로고    scopus 로고
    • Establishment and characterization of 7 novel hepatocellular carcinoma cell lines from patient-derived tumor xenografts
    • Xin H, Wang K, Hu G, Xie F, Ouyang K, Tang X, et al. Establishment and characterization of 7 novel hepatocellular carcinoma cell lines from patient-derived tumor xenografts. PLoS One 2014; 9: e85308.
    • (2014) PLoS One , vol.9
    • Xin, H.1    Wang, K.2    Hu, G.3    Xie, F.4    Ouyang, K.5    Tang, X.6
  • 32
    • 84859097478 scopus 로고    scopus 로고
    • Antibody- mediated inhibition of fibroblast growth factor 19 results in increased bile acids synthesis and ileal malabsorption of bile acids in cynomolgus monkeys
    • Pai R, French D, Ma N, Hotzel K, Plise E, Salphati L, et al. Antibody- mediated inhibition of fibroblast growth factor 19 results in increased bile acids synthesis and ileal malabsorption of bile acids in cynomolgus monkeys. Toxicol Sci Off J Soc Toxicol 2012; 126: 446-56.
    • (2012) Toxicol Sci Off J Soc Toxicol , vol.126 , pp. 446-456
    • Pai, R.1    French, D.2    Ma, N.3    Hotzel, K.4    Plise, E.5    Salphati, L.6
  • 33
    • 34548250374 scopus 로고    scopus 로고
    • A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases
    • Chen H, Ma J, Li W, Eliseenkova AV, Xu C, Neubert TA, et al. A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases. Mol Cell 2007; 27: 717-30.
    • (2007) Mol Cell , vol.27 , pp. 717-730
    • Chen, H.1    Ma, J.2    Li, W.3    Eliseenkova, A.V.4    Xu, C.5    Neubert, T.A.6
  • 34


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.