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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Fibroblast growth factor (FGF) family receptors act as homo- and heterodimers, and are characterized by Ig-like loops in the extracellular domain, in which disulphide bridges may form across protein partners to allow the formation of covalent dimers which may be constitutively active. FGF receptors have been implicated in achondroplasia, angiogenesis and numerous congenital disorders. At least 22 members of the FGF gene family have been identified in the human genome . Within this group, subfamilies of FGF may be divided into canonical, intracellular and hormone-like FGFs. FGF1-FGF10 have been identified to act through FGF receptors, while FGF11-14 appear to signal through intracellular targets. Other family members are less well characterized .
1. Batley BL, Doherty AM, Hamby JM, Lu GH, Keller P, Dahring TK, Hwang O, Crickard K, Panek RL. (1998) Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci., 62 (2): 143-50. [PMID:9488112]
2. Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N et al.. (2015) First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov, 5 (4): 424-37. [PMID:25776529]
3. Liang G, Liu Z, Wu J, Cai Y, Li X. (2012) Anticancer molecules targeting fibroblast growth factor receptors. Trends Pharmacol. Sci., 33 (10): 531-41. [PMID:22884522]
4. Ornitz DM, Xu J, Colvin JS, McEwen DG, MacArthur CA, Coulier F, Gao G, Goldfarb M. (1996) Receptor specificity of the fibroblast growth factor family. J. Biol. Chem., 271 (25): 15292-7. [PMID:8663044]
5. Skaper SD, Kee WJ, Facci L, Macdonald G, Doherty P, Walsh FS. (2000) The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J. Neurochem., 75 (4): 1520-7. [PMID:10987832]
6. Wesche J, Haglund K, Haugsten EM. (2011) Fibroblast growth factors and their receptors in cancer. Biochem. J., 437 (2): 199-213. [PMID:21711248]
7. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K et al.. (2011) 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., 10 (11): 2200-10. [PMID:21900693]
8. Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M et al.. (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem. Biol., 17 (3): 285-95. [PMID:20338520]
Database page citation:
Type V RTKs: FGF (fibroblast growth factor) receptor family. Accessed on 03/12/2016. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=323.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Catalytic receptors. Br J Pharmacol. 172: 5979-6023.