Fibroblast growth factor receptor 4
Also known as: FGFR4, JTK2, TKF
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation of lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism and phosphate homeostasis. Required for normal down-regulation of the expression of CYP7A1, the rate-limiting enzyme in bile acid synthesis, in response to FGF19. Phosphorylates PLCG1 and FRS2. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Promotes SRC-dependent phosphorylation of the matrix protease MMP14 and its lysosomal degradation. FGFR4 signaling is down-regulated by receptor internalization and degradation; MMP14 promotes internalization and degradation of FGFR4. Mutations that lead to constitutive kinase activation or impair normal FGFR4 inactivation lead to aberrant signaling.
Classification
- Family (Pfam)
- PF07679 I-set, PF13927 Ig_3, PF07714 PK_Tyr_Ser-Thr
- InterPro
- FGF_rcpt_fam, Ig-like_dom, Ig-like_dom_sf, Ig-like_fold, Ig_I-set, Ig_sub, Ig_sub2, Kinase-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, RTK, Ser-Thr/Tyr_kinase_cat_dom, Tyr_kinase_AS, Tyr_kinase_cat_dom
- Functional cluster
- Secreted Growth Factors & Cytokines
Experimental structures · PDB · 52
- 4QQ5 X-ray 2.20A
- 4QQC X-ray 2.40A
- 4QQJ X-ray 1.68A
- 4QQT X-ray 1.50A
- 4QRC X-ray 1.90A
- 4R6V X-ray 2.35A
- 4TYE X-ray 2.80A
- 4TYG X-ray 2.40A
- 4TYI X-ray 3.40A
- 4TYJ X-ray 2.45A
- 4UXQ X-ray 1.85A
- 4XCU X-ray 1.71A
- … and 40 more
A predicted model is available from AlphaFold.
Gene Ontology · 27
- GO:0005783 endoplasmic reticulum
- GO:0005768 endosome
- GO:0005576 extracellular region
- GO:0005794 Golgi apparatus
- GO:0005886 plasma membrane
- GO:0043235 receptor complex
- GO:0030133 transport vesicle
- GO:0005524 ATP binding
- GO:0017134 fibroblast growth factor binding
- GO:0005007 fibroblast growth factor receptor activity
- GO:0008201 heparin binding
- GO:0016477 cell migration
- GO:0042632 cholesterol homeostasis
- GO:0008543 fibroblast growth factor receptor signaling pathway
- GO:0042593 glucose homeostasis
- GO:0018108 peptidyl-tyrosine phosphorylation
- GO:0055062 phosphate ion homeostasis
- GO:0043085 positive regulation of catalytic activity
- GO:0008284 positive regulation of cell population proliferation
- GO:2000573 positive regulation of DNA biosynthetic process
- GO:0070374 positive regulation of ERK1 and ERK2 cascade
- GO:0010628 positive regulation of gene expression
- GO:0045862 positive regulation of proteolysis
- GO:0046777 protein autophosphorylation
- GO:0070857 regulation of bile acid biosynthetic process
- GO:0010715 regulation of extracellular matrix disassembly
- GO:0019216 regulation of lipid metabolic process
Drugs targeting this protein · 15
- INFIGRATINIB PHOSPHATE inhibitor
- INFIGRATINIB inhibitor
- BRIVANIB ALANINATE inhibitor
- ORANTINIB inhibitor
- NINTEDANIB ESYLATE inhibitor
- FEXAGRATINIB inhibitor
- ERDAFITINIB inhibitor
- FUTIBATINIB inhibitor
- BRIVANIB inhibitor
- LY-2874455 inhibitor
- FGF401 inhibitor
- ROGARATINIB inhibitor
- DERAZANTINIB inhibitor
- ENMD-981693 inhibitor
- XL-999 inhibitor
Related proteins · sequence + function similarity
- Fibroblast growth factor receptor 4 0.98
- Fibroblast growth factor receptor 4 0.97
- Tyrosine-protein kinase receptor TYRO3 0.85
- Tyrosine-protein kinase receptor TYRO3 0.85
- Tyrosine-protein kinase receptor UFO 0.84
- Tyrosine-protein kinase receptor TYRO3 0.84
- Fibroblast growth factor receptor 3 0.83
- Fibroblast growth factor receptor 3 0.83
- High affinity nerve growth factor receptor 0.81
- Ephrin type-B receptor 6 0.81
- High affinity nerve growth factor receptor 0.81
- Ephrin type-B receptor 6 0.81
Co-cited proteins · studied together in the literature
- Fibroblast growth factor receptor 1 7 shared papers
- Fibroblast growth factor receptor 3 7 shared papers
- Fibroblast growth factor receptor 4 1 shared papers
- Fibroblast growth factor receptor 4 1 shared papers
- Fibroblast growth factor receptor 2 6 shared papers
- 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 1 shared papers
- Phosphatidylinositol 3-kinase regulatory subunit alpha 1 shared papers
- Fibroblast growth factor 19 3 shared papers
- Fibroblast growth factor 7 3 shared papers
- Fibroblast growth factor 9 3 shared papers
- Fibroblast growth factor 21 2 shared papers
- Fibroblast growth factor 3 2 shared papers
Literature · 36 cited papers
- Germline variant FGFR4 p.G388R exposes a membrane-proximal STAT3 binding site. Nature · 2015
- PMID 26237043 J. Clin. Invest. · 2015
- An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. J. Proteomics · 2014
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- PAX3-FOXO1 and FGFR4 in alveolar rhabdomyosarcoma. Mol. Carcinog. · 2012
- Sulfated glycosaminoglycans are required for specific and sensitive fibroblast growth factor (FGF) 19 signaling via FGF receptor 4 and betaKlotho. J. Biol. Chem. · 2011
- Meta and pooled analyses of FGFR4 Gly388Arg polymorphism as a cancer prognostic factor. Eur. J. Cancer Prev. · 2011
- FGFR4 Gly388Arg polymorphism contributes to prostate cancer development and progression: a meta-analysis of 2618 cases and 2305 controls. BMC Cancer · 2011
- Initial characterization of the human central proteome. BMC Syst. Biol. · 2011
- Fibroblast growth factor receptor 4 regulates tumor invasion by coupling fibroblast growth factor signaling to extracellular matrix degradation. Cancer Res. · 2010
- FGF receptor-4 (FGFR4) polymorphism acts as an activity switch of a membrane type 1 matrix metalloproteinase-FGFR4 complex. Proc. Natl. Acad. Sci. U.S.A. · 2010
- Glycosylation of fibroblast growth factor receptor 4 is a key regulator of fibroblast growth factor 19-mediated down-regulation of cytochrome P450 7A1. Hepatology · 2010
- … and 24 more in the literature graph