Fibroblast Growth Factor Receptor 4 Targeting in Cancer: New Insights into Mechanisms and Therapeutic Strategies.

作者: Liwei Lang , Yong Teng

DOI: 10.3390/CELLS8010031

关键词: FGF19Cell growthFibroblast growth factorCancerCancer researchRegulation of gene expressionFibroblast growth factor receptor 4OncogeneReceptor tyrosine kinaseBiology

摘要: Fibroblast growth factor receptor 4 (FGFR4), a tyrosine kinase for FGFs, is involved in diverse cellular processes, including the regulation of cell proliferation, differentiation, migration, metabolism, and bile acid biosynthesis. High activation FGFR4 strongly associated with amplification its specific ligand FGF19 many types solid tumors hematologic malignancies, where it acts as an oncogene driving cancer development progression. Currently, therapeutic evaluation FGFR4-specific inhibitors, such BLU9931 H3B-6527, animal models patients, are paving way to suppress hyperactive signaling cancer. This comprehensive review not only covers recent discoveries understanding function cancer, but also reveals implications applications regarding emerging anti-FGFR4 agents. Our aim pinpoint potential target identify new avenues advancing future research field.

参考文章(67)
Ashraf Dallol, Abdelbaset Buhmeida, Adnan Merdad, Jaudah Al-Maghrabi, Mamdooh A. Gari, Muhammad M. Abu-Elmagd, Aisha Elaimi, Mourad Assidi, Adeel G. Chaudhary, Adel M. Abuzenadah, Taoufik Nedjadi, Eramah Ermiah, Shadi S. Alkhayyat, Mohammed H. Al-Qahtani, Frequent methylation of the KLOTHO gene and overexpression of the FGFR4 receptor in invasive ductal carcinoma of the breast. Tumor Biology. ,vol. 36, pp. 9677- 9683 ,(2015) , 10.1007/S13277-015-3733-3
Nadia Panera, Sara Ceccarelli, Valerio Nobili, Anna Alisi, Targeting FGF19 binding to its receptor system: A novel therapeutic approach for hepatocellular carcinoma Hepatology. ,vol. 62, pp. 1324- 1324 ,(2015) , 10.1002/HEP.27741
Maria E. Cabanillas, Martin Schlumberger, Barbara Jarzab, Renato G. Martins, Furio Pacini, Bruce Robinson, Judith C. McCaffrey, Manisha H. Shah, Donald L. Bodenner, Duncan Topliss, Corina Andresen, James P. O'Brien, Min Ren, Yasuhiro Funahashi, Roger Allison, Rossella Elisei, Kate Newbold, Lisa F. Licitra, Steven I. Sherman, Douglas W. Ball, A phase 2 trial of lenvatinib (E7080) in advanced, progressive, radioiodine-refractory, differentiated thyroid cancer: A clinical outcomes and biomarker assessment. Cancer. ,vol. 121, pp. 2749- 2756 ,(2015) , 10.1002/CNCR.29395
Teresa Helsten, Maria Schwaederle, Razelle Kurzrock, Fibroblast growth factor receptor signaling in hereditary and neoplastic disease: biologic and clinical implications Cancer and Metastasis Reviews. ,vol. 34, pp. 479- 496 ,(2015) , 10.1007/S10555-015-9579-8
Jakob Paur, Lisa Nika, Christiane Maier, Alexander Moscu-Gregor, Julia Kostka, Daniela Huber, Thomas Mohr, Petra Heffeter, Waltraud C. Schrottmaier, Sonja Kappel, Daniela Kandioler, Klaus Holzmann, Brigitte Marian, Walter Berger, Michael Grusch, Bettina Grasl-Kraupp, Fibroblast growth factor receptor 3 isoforms: Novel therapeutic targets for hepatocellular carcinoma? Hepatology. ,vol. 62, pp. 1767- 1778 ,(2015) , 10.1002/HEP.28023
Juha Partanen, TP Mäkelä, Elina Eerola, Jaana Korhonen, H Hirvonen, L Claesson‐Welsh, K Alitalo, None, FGFR-4, a novel acidic fibroblast growth factor receptor with a distinct expression pattern. The EMBO Journal. ,vol. 10, pp. 1347- 1354 ,(1991) , 10.1002/J.1460-2075.1991.TB07654.X
Teresa Helsten, Sheryl Elkin, Elisa Arthur, Brett N. Tomson, Jennifer Carter, Razelle Kurzrock, The FGFR Landscape in Cancer: Analysis of 4,853 Tumors by Next-Generation Sequencing Clinical Cancer Research. ,vol. 22, pp. 259- 267 ,(2016) , 10.1158/1078-0432.CCR-14-3212
Alberto Peláez-García, Rodrigo Barderas, Sofía Torres, Pablo Hernández-Varas, Joaquín Teixidó, Félix Bonilla, Antonio Garcia de Herreros, J. Ignacio Casal, FGFR4 Role in Epithelial-Mesenchymal Transition and Its Therapeutic Value in Colorectal Cancer PLOS ONE. ,vol. 8, ,(2013) , 10.1371/JOURNAL.PONE.0063695
Serkan Kir, Sara A Beddow, Varman T Samuel, Paul Miller, Stephen F Previs, Kelly Suino-Powell, H Eric Xu, Gerald I Shulman, Steven A Kliewer, David J Mangelsdorf, FGF19 as a Postprandial, Insulin-Independent Activator of Hepatic Protein and Glycogen Synthesis Science. ,vol. 331, pp. 1621- 1624 ,(2011) , 10.1126/SCIENCE.1198363