FGFR1

Summary

Gene Symbol: FGFR1
Description: fibroblast growth factor receptor 1
Alias: BFGFR, CD331, CEK, ECCL, FGFBR, FGFR-1, FLG, FLT-2, FLT2, HBGFR, HH2, HRTFDS, KAL2, N-SAM, OGD, bFGF-R-1, fibroblast growth factor receptor 1, FGFR1/PLAG1 fusion, FMS-like tyrosine kinase 2, basic fibroblast growth factor receptor 1, fms-related tyrosine kinase 2, heparin-binding growth factor receptor, hydroxyaryl-protein kinase, proto-oncogene c-Fgr
Species: human
Products:     FGFR1

Top Publications

  1. Eswarakumar V, Lax I, Schlessinger J. Cellular signaling by fibroblast growth factor receptors. Cytokine Growth Factor Rev. 2005;16:139-49 pubmed
    ..binding to and activating the different isoforms encoded by the four receptor tyrosine kinases (RTKs) designated FGFR1, FGFR2, FGFR3 and FGFR4...
  2. Tsimafeyeu I, Demidov L, Stepanova E, Wynn N, Ta H. Overexpression of fibroblast growth factor receptors FGFR1 and FGFR2 in renal cell carcinoma. Scand J Urol Nephrol. 2011;45:190-5 pubmed publisher
    ..This study evaluated the expression of FGFR1 and FGFR2 in RCC...
  3. Mohammadi M, Dionne C, Li W, Li N, Spivak T, Honegger A, et al. Point mutation in FGF receptor eliminates phosphatidylinositol hydrolysis without affecting mitogenesis. Nature. 1992;358:681-4 pubmed
  4. Groth C, Lardelli M. The structure and function of vertebrate fibroblast growth factor receptor 1. Int J Dev Biol. 2002;46:393-400 pubmed
    The vertebrate fibroblast growth factor receptor 1 (FGFR1) is alternatively spliced generating multiple splice variants that are differentially expressed during embryo development and in the adult body...
  5. Issa A, Gill J, Heideman M, Sahin O, Wiemann S, Dey J, et al. Combinatorial targeting of FGF and ErbB receptors blocks growth and metastatic spread of breast cancer models. Breast Cancer Res. 2013;15:R8 pubmed publisher
    ..Considering that sub-classes of human breast tumors co-express ErbB receptors and FGFRs, these results have implications for targeted therapy. ..
  6. Stachowiak E, Maher P, Tucholski J, Mordechai E, Joy A, Moffett J, et al. Nuclear accumulation of fibroblast growth factor receptors in human glial cells--association with cell proliferation. Oncogene. 1997;14:2201-11 pubmed
    ..of total cell extracts with FGF receptor (FGFR) 1-4 antibodies showed that U251MG glioma cells express only FGFR1. [125I]FGF-2 cross linking to nuclear extracts followed by FGFR1 immunoprecipitation showed that FGFR1 may account ..
  7. Ong S, Hadari Y, Gotoh N, Guy G, Schlessinger J, Lax I. Stimulation of phosphatidylinositol 3-kinase by fibroblast growth factor receptors is mediated by coordinated recruitment of multiple docking proteins. Proc Natl Acad Sci U S A. 2001;98:6074-9 pubmed
  8. Lew E, Furdui C, Anderson K, Schlessinger J. The precise sequence of FGF receptor autophosphorylation is kinetically driven and is disrupted by oncogenic mutations. Sci Signal. 2009;2:ra6 pubmed publisher
    Autophosphorylation of the tyrosine kinase domain of fibroblast growth factor receptor 1 (FGFR1) is mediated by a sequential and precisely ordered three-stage autophosphorylation reaction...
  9. Bryant D, Wylie F, Stow J. Regulation of endocytosis, nuclear translocation, and signaling of fibroblast growth factor receptor 1 by E-cadherin. Mol Biol Cell. 2005;16:14-23 pubmed
    ..In this study, we investigated the location, trafficking, and function of FGFR1 and E-cadherin and report a novel mechanism, based on endocytic trafficking, for the coregulation of E-cadherin ..

More Information

Publications89

  1. Leung H, Gullick W, Lemoine N. Expression and functional activity of fibroblast growth factors and their receptors in human pancreatic cancer. Int J Cancer. 1994;59:667-75 pubmed
    ..Treatment of monolayer cultures of the same cell lines did not promote growth. However, a specific neutralising antibody against FGF-2 reduced cell proliferation of MIA PACA-2 cells by 50%. ..
  2. Raivio T, Avbelj M, McCabe M, Romero C, Dwyer A, Tommiska J, et al. Genetic overlap in Kallmann syndrome, combined pituitary hormone deficiency, and septo-optic dysplasia. J Clin Endocrinol Metab. 2012;97:E694-9 pubmed publisher
    ..Kallmann syndrome (KS), combined pituitary hormone deficiency (CPHD), and septo-optic dysplasia (SOD) all result from development defects of the anterior midline in the human forebrain...
  3. Tran T, Selinger C, Kohonen Corish M, McCaughan B, Kennedy C, O Toole S, et al. Fibroblast growth factor receptor 1 (FGFR1) copy number is an independent prognostic factor in non-small cell lung cancer. Lung Cancer. 2013;81:462-7 pubmed publisher
    b>Fibroblast growth factor receptor 1 (FGFR1) is an oncogene that can potentially be targeted by tyrosine kinase inhibitors...
  4. Stachowiak M, Maher P, Joy A, Mordechai E, Stachowiak E. Nuclear localization of functional FGF receptor 1 in human astrocytes suggests a novel mechanism for growth factor action. Brain Res Mol Brain Res. 1996;38:161-5 pubmed
    Fractionation of human astrocytes revealed the presence of 103, 118, and 145 kDa forms of FGF receptor 1 (FGFR1) in isolated nuclei. Only trace amounts of FGFR1 proteins were detected in the cell membrane or cytoplasmic fractions...
  5. Schildhaus H, Heukamp L, Merkelbach Bruse S, Riesner K, Schmitz K, Binot E, et al. Definition of a fluorescence in-situ hybridization score identifies high- and low-level FGFR1 amplification types in squamous cell lung cancer. Mod Pathol. 2012;25:1473-80 pubmed publisher
    We recently reported fibroblast growth factor receptor-type 1 (FGFR1) amplification to be associated with therapeutically tractable FGFR1 dependency in squamous cell lung cancer...
  6. Guimarães J, Guimarães I, Duarte M, Vieira T, Vianna V, Fernandes M, et al. Polymorphisms in BMP4 and FGFR1 genes are associated with fracture non-union. J Orthop Res. 2013;31:1971-9 pubmed publisher
    ..A total of 16 SNPs within five genes involved in bone repair pathogenesis (FAM5C, BMP4, FGF3, FGF10, and FGFR1) were investigated in 167 patients with long bone fractures, 101 with uneventful healing, and 66 presenting ..
  7. Pitteloud N, Acierno J, Meysing A, Dwyer A, Hayes F, Crowley W. Reversible kallmann syndrome, delayed puberty, and isolated anosmia occurring in a single family with a mutation in the fibroblast growth factor receptor 1 gene. J Clin Endocrinol Metab. 2005;90:1317-22 pubmed
    ..Recently, loss-of-function mutations in the fibroblast growth factor receptor 1 (FGFR1) gene have been shown to cause autosomal dominant KS...
  8. Popovici C, Zhang B, Gregoire M, Jonveaux P, Lafage Pochitaloff M, Birnbaum D, et al. The t(6;8)(q27;p11) translocation in a stem cell myeloproliferative disorder fuses a novel gene, FOP, to fibroblast growth factor receptor 1. Blood. 1999;93:1381-9 pubmed
    ..The t(8;13) translocation has recently been shown to result in a fusion between the FGFR1 gene that encodes a tyrosine kinase receptor for fibroblast growth factors and a novel gene, FIM (also called RAMP ..
  9. Jarzabek K, Wolczynski S, Lesniewicz R, Plessis G, Kottler M. Evidence that FGFR1 loss-of-function mutations may cause variable skeletal malformations in patients with Kallmann syndrome. Adv Med Sci. 2012;57:314-21 pubmed publisher
    Loss-of-function mutations in FGFR1 have been identified in approximately 10% of the Kallmann syndrome (KS) patients...
  10. Dutt A, Ramos A, Hammerman P, Mermel C, Cho J, Sharifnia T, et al. Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS ONE. 2011;6:e20351 pubmed publisher
    ..array analysis, we found that a region of chromosome segment 8p11-12 containing three genes-WHSC1L1, LETM2, and FGFR1-is amplified in 3% of lung adenocarcinomas and 21% of squamous cell lung carcinomas...
  11. Dong S, Kang S, Gu T, Kardar S, Fu H, Lonial S, et al. 14-3-3 Integrates prosurvival signals mediated by the AKT and MAPK pathways in ZNF198-FGFR1-transformed hematopoietic cells. Blood. 2007;110:360-9 pubmed
    ..The syndrome associated with t(8;13)(p11;q12) results in expression of the ZNF198-FGFR1 fusion tyrosine kinase that plays a pathogenic role in hematopoietic transformation...
  12. Oxnard G, Binder A, Janne P. New targetable oncogenes in non-small-cell lung cancer. J Clin Oncol. 2013;31:1097-104 pubmed publisher
    ..alterations have been characterized in recent years, including BRAF mutations, HER2 insertions, PIK3CA mutations, FGFR1 amplifications, DDR2 mutations, ROS1 rearrangements, and RET rearrangements...
  13. Sørensen V, Zhen Y, Zakrzewska M, Haugsten E, Walchli S, Nilsen T, et al. Phosphorylation of fibroblast growth factor (FGF) receptor 1 at Ser777 by p38 mitogen-activated protein kinase regulates translocation of exogenous FGF1 to the cytosol and nucleus. Mol Cell Biol. 2008;28:4129-41 pubmed publisher
    ..The activity level of p38 MAPK was not found to affect endocytosis or intracellular sorting of FGF1/FGFR1. Instead, we found that p38 MAPK regulates FGF1 translocation by phosphorylation of FGFR1 at Ser777...
  14. Kim H, Kim D, Kang D, Lee J, Lim S, Lee C, et al. Fibroblast growth factor receptor 1 gene amplification is associated with poor survival and cigarette smoking dosage in patients with resected squamous cell lung cancer. J Clin Oncol. 2013;31:731-7 pubmed publisher
    To investigate the frequency and the prognostic role of fibroblast growth factor receptor 1 (FGFR1) amplification in patients with surgically resected squamous cell carcinoma of the lung (SCCL) and the association between smoking and ..
  15. Weiss J, Sos M, Seidel D, Peifer M, Zander T, Heuckmann J, et al. Frequent and focal FGFR1 amplification associates with therapeutically tractable FGFR1 dependency in squamous cell lung cancer. Sci Transl Med. 2010;2:62ra93 pubmed publisher
    ..We identified frequent and focal fibroblast growth factor receptor 1 (FGFR1) amplification in squamous cell lung cancer (n = 155), but not in other lung cancer subtypes,..
  16. Sharpe R, Pearson A, Herrera Abreu M, Johnson D, Mackay A, Welti J, et al. FGFR signaling promotes the growth of triple-negative and basal-like breast cancer cell lines both in vitro and in vivo. Clin Cancer Res. 2011;17:5275-86 pubmed publisher
    ..Basal-like breast cancer cell lines, and breast cancers, express autocrine FGF2 and show sensitivity to FGFR inhibitors, identifying a potential novel therapeutic approach for these cancers. ..
  17. Chen G, Tian X, Liu Z, Zhou S, Schmidt B, Henne Bruns D, et al. Inhibition of endogenous SPARC enhances pancreatic cancer cell growth: modulation by FGFR1-III isoform expression. Br J Cancer. 2010;102:188-95 pubmed publisher
    ..Endogenous SPARC expression in PANC-1 cells was increased in FGFR1-IIIb over-expressing cells, but decreased in FGFR1-IIIc over-expressing cells...
  18. Bhide R, Lombardo L, Hunt J, Cai Z, Barrish J, Galbraith S, et al. The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases. Mol Cancer Ther. 2010;9:369-78 pubmed publisher
    ..These results show that brivanib alaninate is an effective antitumor agent in preclinical models across a range of doses, and that efficacy is accompanied by changes in cellular and vascular activities. ..
  19. Urakawa I, Yamazaki Y, Shimada T, Iijima K, Hasegawa H, Okawa K, et al. Klotho converts canonical FGF receptor into a specific receptor for FGF23. Nature. 2006;444:770-4 pubmed
    ..to be incapable of intracellular signalling, we searched for other components of the FGF23 receptor and found FGFR1(IIIc), which was directly converted by Klotho into the FGF23 receptor...
  20. Riley B, Mansilla M, Ma J, Daack Hirsch S, Maher B, Raffensperger L, et al. Impaired FGF signaling contributes to cleft lip and palate. Proc Natl Acad Sci U S A. 2007;104:4512-7 pubmed
    ..We sequenced the coding regions and performed association testing on 12 genes (FGFR1, FGFR2, FGFR3, FGF2, FGF3, FGF4, FGF7, FGF8, FGF9, FGF10, FGF18, and NUDT6) and used protein structure analyses to ..
  21. Dode C, Fouveaut C, Mortier G, Janssens S, Bertherat J, Mahoudeau J, et al. Novel FGFR1 sequence variants in Kallmann syndrome, and genetic evidence that the FGFR1c isoform is required in olfactory bulb and palate morphogenesis. Hum Mutat. 2007;28:97-8 pubmed
    In a new cohort of 141 unrelated patients affected by Kallmann syndrome we identified FGFR1 sequence variants in 17 patients, all in the heterozygous state. The fifteen novel variants consist of 10 missense (p.N77K, p.C101F, p.R250W, p...
  22. Singh D, Chan J, Zoppoli P, Niola F, Sullivan R, Castaño A, et al. Transforming fusions of FGFR and TACC genes in human glioblastoma. Science. 2012;337:1231-5 pubmed publisher
    ..that fuse in-frame the tyrosine kinase coding domains of fibroblast growth factor receptor (FGFR) genes (FGFR1 or FGFR3) to the transforming acidic coiled-coil (TACC) coding domains of TACC1 or TACC3, respectively...
  23. Wasag B, Lierman E, Meeus P, Cools J, Vandenberghe P. The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11). Haematologica. 2011;96:922-6 pubmed publisher
    ..CUX1 was identified as the fusion partner of FGFR1 by fluorescence in situ hybridization and 5' RACE-PCR...
  24. Tomlinson D, Lamont F, Shnyder S, Knowles M. Fibroblast growth factor receptor 1 promotes proliferation and survival via activation of the mitogen-activated protein kinase pathway in bladder cancer. Cancer Res. 2009;69:4613-20 pubmed publisher
    ..normal human urothelial cells, urothelial carcinoma cell lines, and tumor samples and showed that FGFR1 expression is increased in a high proportion of cell lines and tumors independent of stage and grade...
  25. Bae J, Lew E, Yuzawa S, Tomé F, Lax I, Schlessinger J. The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site. Cell. 2009;138:514-24 pubmed publisher
    ..Here we describe the crystal structure of the activated tyrosine kinase domain of FGFR1 in complex with a phospholipase Cgamma fragment...
  26. Freier K, Schwaenen C, Sticht C, Flechtenmacher C, Mühling J, Hofele C, et al. Recurrent FGFR1 amplification and high FGFR1 protein expression in oral squamous cell carcinoma (OSCC). Oral Oncol. 2007;43:60-6 pubmed
    ..Furthermore, a distinct high-level amplification of the fibroblast growth factor receptor 1 (FGFR1) locus was detected in two cases...
  27. Schlessinger J, Plotnikov A, Ibrahimi O, Eliseenkova A, Yeh B, Yayon A, et al. Crystal structure of a ternary FGF-FGFR-heparin complex reveals a dual role for heparin in FGFR binding and dimerization. Mol Cell. 2000;6:743-50 pubmed
    ..This model provides a structural basis for FGFR activation by small molecule heparin analogs and may facilitate the design of heparin mimetics capable of modulating FGF signaling. ..
  28. Luqmani Y, Graham M, Coombes R. Expression of basic fibroblast growth factor, FGFR1 and FGFR2 in normal and malignant human breast, and comparison with other normal tissues. Br J Cancer. 1992;66:273-80 pubmed
    The expression of basic fibroblast growth factor (bFGF) and two of its receptors, FGFR1 and FGFR2, was detected using the polymerase chain reaction, and quantified by comparison to the relative amount of product obtained following co-..
  29. Ornitz D, Xu J, Colvin J, McEwen D, MacArthur C, Coulier F, et al. Receptor specificity of the fibroblast growth factor family. J Biol Chem. 1996;271:15292-7 pubmed
    ..These data should serve as a biochemical foundation for determining developmental, physiological, and pathophysiological processes that involve FGF signaling pathways. ..
  30. Levi E, Fridman R, Miao H, Ma Y, Yayon A, Vlodavsky I. Matrix metalloproteinase 2 releases active soluble ectodomain of fibroblast growth factor receptor 1. Proc Natl Acad Sci U S A. 1996;93:7069-74 pubmed
    Recent studies have demonstrated the existence of a soluble fibroblast growth factor (FGF) receptor type 1 (FGFR1) extracellular domain in the circulation and in vascular basement membranes...
  31. Schultheis A, Bos M, Schmitz K, Wilsberg L, Binot E, Wolf J, et al. Fibroblast growth factor receptor 1 (FGFR1) amplification is a potential therapeutic target in small-cell lung cancer. Mod Pathol. 2014;27:214-21 pubmed publisher
    ..In this study we analyzed a cohort of 307 SCLC samples for fibroblast growth factor receptor 1 (FGFR1) amplification using a dual color FISH probe. FGFR1 status was correlated with clinical data...
  32. DiGabriele A, Lax I, Chen D, Svahn C, Jaye M, Schlessinger J, et al. Structure of a heparin-linked biologically active dimer of fibroblast growth factor. Nature. 1998;393:812-7 pubmed
    ..The dimerization of heparin-linked acidic FGF observed here is an elegant mechanism for the modulation of signalling through combinatorial homodimerization and heterodimerization of the 12 known members of the FGF family. ..
  33. Kan M, Wu X, Wang F, McKeehan W. Specificity for fibroblast growth factors determined by heparan sulfate in a binary complex with the receptor kinase. J Biol Chem. 1999;274:15947-52 pubmed
    ..FGFR type 4 (FGFR4) in liver parenchymal cells binds only FGF-1, whereas FGFR1 binds FGF-1 and FGF-2 equally. Cell-free complexes of heparin and recombinant FGFR4 bound FGF-1 and FGF-2 equally...
  34. Reilly J, Mickey G, Maher P. Association of fibroblast growth factor receptor 1 with the adaptor protein Grb14. Characterization of a new receptor binding partner. J Biol Chem. 2000;275:7771-8 pubmed
    Using the cytoplasmic domain of fibroblast growth factor receptor 1 (FGFR1) as bait in a yeast two-hybrid screen, Grb14 was identified as a FGFR1 binding partner...
  35. Young R, Lim A, Angel C, Collins M, Deb S, Corry J, et al. Frequency of fibroblast growth factor receptor 1 gene amplification in oral tongue squamous cell carcinomas and associations with clinical features and patient outcome. Oral Oncol. 2013;49:576-81 pubmed publisher
    ..b>Fibroblast Growth Factor Receptor 1 (FGFR1) amplification frequently occurs in squamous cell carcinoma of the lung and represents a ..
  36. Kos F, Chin C. Costimulation of T cell receptor-triggered IL-2 production by Jurkat T cells via fibroblast growth factor receptor 1 upon its engagement by CD56. Immunol Cell Biol. 2002;80:364-9 pubmed
    ..We demonstrate that ligation of FGFR1 beta on J.C2-14 Jurkat T cells by CD56 on fixed NK-92 cells costimulates TCR/CD3-triggered IL-2 production...
  37. Dode C, Levilliers J, Dupont J, De Paepe A, Le Dû N, Soussi Yanicostas N, et al. Loss-of-function mutations in FGFR1 cause autosomal dominant Kallmann syndrome. Nat Genet. 2003;33:463-5 pubmed
    ..We establish here that loss-of-function mutations in FGFR1 underlie KAL2 whereas a gain-of-function mutation in FGFR1 has been shown to cause a form of craniosynostosis...
  38. Kiselyov V, Skladchikova G, Hinsby A, Jensen P, Kulahin N, Soroka V, et al. Structural basis for a direct interaction between FGFR1 and NCAM and evidence for a regulatory role of ATP. Structure. 2003;11:691-701 pubmed
    ..demonstrate for the first time a direct interaction between NCAM (fibronectin type III [F3] modules 1 and 2) and FGFR1 (Ig modules 2 and 3) by surface plasmon resonance (SPR) analysis...
  39. Kohler L, Mireskandari M, Knösel T, Altendorf Hofmann A, Kunze A, Schmidt A, et al. FGFR1 expression and gene copy numbers in human lung cancer. Virchows Arch. 2012;461:49-57 pubmed publisher
    b>FGFR1 is a receptor tyrosine kinase of which the ligands belong to the fibroblast growth factor family...
  40. Borroto Escuela D, Romero Fernandez W, Mudo G, Perez Alea M, Ciruela F, Tarakanov A, et al. Fibroblast growth factor receptor 1- 5-hydroxytryptamine 1A heteroreceptor complexes and their enhancement of hippocampal plasticity. Biol Psychiatry. 2012;71:84-91 pubmed publisher
    ..Using bioluminescence resonance energy transfer analysis, fibroblast growth factor receptor 1 (FGFR1)-5-hydroxytryptamine 1A (5-HT1A) receptor complexes have been demonstrated and their ..
  41. Bunney T, Esposito D, Mas Droux C, Lamber E, Baxendale R, Martins M, et al. Structural and functional integration of the PLC? interaction domains critical for regulatory mechanisms and signaling deregulation. Structure. 2012;20:2062-75 pubmed publisher
  42. Laitinen E, Vaaralahti K, Tommiska J, Eklund E, Tervaniemi M, Valanne L, et al. Incidence, phenotypic features and molecular genetics of Kallmann syndrome in Finland. Orphanet J Rare Dis. 2011;6:41 pubmed publisher
    ..Its exact incidence is currently unknown, and a mutation in one of the identified KS genes has only been found in ~30% of the patients...
  43. Wynes M, Hinz T, Gao D, Martini M, Marek L, Ware K, et al. FGFR1 mRNA and protein expression, not gene copy number, predict FGFR TKI sensitivity across all lung cancer histologies. Clin Cancer Res. 2014;20:3299-309 pubmed publisher
    b>FGFR1 gene copy number (GCN) is being evaluated as a biomarker for FGFR tyrosine kinase inhibitor (TKI) response in squamous cell lung cancers (SCC)...
  44. Tomlinson D, Baxter E, Loadman P, Hull M, Knowles M. FGFR1-induced epithelial to mesenchymal transition through MAPK/PLC?/COX-2-mediated mechanisms. PLoS ONE. 2012;7:e38972 pubmed publisher
    ..We have demonstrated that FGFR1 expression is increased in bladder cancer and that activation of FGFR1 induces an EMT in urothelial carcinoma (UC) ..
  45. Tomlinson D, Knowles M. Altered splicing of FGFR1 is associated with high tumor grade and stage and leads to increased sensitivity to FGF1 in bladder cancer. Am J Pathol. 2010;177:2379-86 pubmed publisher
    ..Previously, we demonstrated that FGFR1 expression is increased in urothelial carcinoma cell lines and tumors, which promotes proliferation and survival ..
  46. Chamorro Jorganes A, Araldi E, Penalva L, Sandhu D, Fernandez Hernando C, Suarez Y. MicroRNA-16 and microRNA-424 regulate cell-autonomous angiogenic functions in endothelial cells via targeting vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1. Arterioscler Thromb Vasc Biol. 2011;31:2595-606 pubmed publisher
    ..Vascular endothelial growth factor (VEGF), VEGF receptor-2 (VEGFR2), and fibroblast growth factor receptor-1 (FGFR1) were identified by bioinformatic approaches and subsequently validated as targets of microRNA (miR)-16 and miR-..
  47. Wilkie A. Bad bones, absent smell, selfish testes: the pleiotropic consequences of human FGF receptor mutations. Cytokine Growth Factor Rev. 2005;16:187-203 pubmed
    ..Amongst the most interesting recent discoveries have been the description of novel phenotypes associated with FGFR1 and FGFR3 mutations; identification of fundamental differences in the cellular mechanisms of mutant FGFR2 and ..
  48. Sorokin A, Mohammadi M, Huang J, Schlessinger J. Internalization of fibroblast growth factor receptor is inhibited by a point mutation at tyrosine 766. J Biol Chem. 1994;269:17056-61 pubmed
    ..Wild-type FGF receptor 1 (flg) and a mutated receptor (Y766F), in which an autophosphorylation site (Tyr-766) was mutated to phenylalanine, were ..
  49. Plotnikov A, Hubbard S, Schlessinger J, Mohammadi M. Crystal structures of two FGF-FGFR complexes reveal the determinants of ligand-receptor specificity. Cell. 2000;101:413-24 pubmed
    ..FGF2 complexed with the ligand binding domains (immunoglobulin-like domains 2 [D2] and 3 [D3]) of FGF receptor 1 (FGFR1) and FGFR2, respectively...
  50. Reilly J, Maher P. Importin beta-mediated nuclear import of fibroblast growth factor receptor: role in cell proliferation. J Cell Biol. 2001;152:1307-12 pubmed
    ..Furthermore, we show that nuclear FGFR1 induces c-Jun and is involved in the regulation of cell proliferation...
  51. Baumann H, Kunapuli P, Tracy E, Cowell J. The oncogenic fusion protein-tyrosine kinase ZNF198/fibroblast growth factor receptor-1 has signaling function comparable with interleukin-6 cytokine receptors. J Biol Chem. 2003;278:16198-208 pubmed
    ..the zinc finger protein ZNF198 is combined with the cytoplasmic domain of the fibroblast growth factor receptor-1 (FGFR1)...
  52. Somanathan S, Stachowiak E, Siegel A, Stachowiak M, Berezney R. Nuclear matrix bound fibroblast growth factor receptor is associated with splicing factor rich and transcriptionally active nuclear speckles. J Cell Biochem. 2003;90:856-69 pubmed
    ..functional significance of a constitutively expressed form of the receptor tyrosine kinase FGFR1 (fibroblast growth factor receptor 1) in the nucleus of rapidly proliferating serum stimulated TE 671 cells, a medullobastoma human cell ..
  53. Ibrahimi O, Zhang F, Hrstka S, Mohammadi M, Linhardt R. Kinetic model for FGF, FGFR, and proteoglycan signal transduction complex assembly. Biochemistry. 2004;43:4724-30 pubmed
    ..The recent FGF2-FGFR1-heparin crystal structure provides a detailed but static view of the FGF-FGFR-heparin complex...
  54. Fang X, Stachowiak E, Dunham Ems S, Klejbor I, Stachowiak M. Control of CREB-binding protein signaling by nuclear fibroblast growth factor receptor-1: a novel mechanism of gene regulation. J Biol Chem. 2005;280:28451-62 pubmed
    In integrative nuclear fibroblast growth factor receptor-1 (FGFR1) signaling a newly synthesized FGFR1 translocates to the nucleus to stimulate cell differentiation and associated gene activities...
  55. Abreu A, Trarbach E, de Castro M, Frade Costa E, Versiani B, Matias Baptista M, et al. Loss-of-function mutations in the genes encoding prokineticin-2 or prokineticin receptor-2 cause autosomal recessive Kallmann syndrome. J Clin Endocrinol Metab. 2008;93:4113-8 pubmed publisher
    ..Physiological activation of the prokineticin pathway has a critical role in olfactory bulb morphogenesis and GnRH secretion in mice...
  56. Trarbach E, Costa E, Versiani B, de Castro M, Baptista M, Garmes H, et al. Novel fibroblast growth factor receptor 1 mutations in patients with congenital hypogonadotropic hypogonadism with and without anosmia. J Clin Endocrinol Metab. 2006;91:4006-12 pubmed
    ..To date, loss-of-function mutations in the genes encoding anosmin-1 (KAL1) and fibroblast growth factor receptor 1 (FGFR1) have been described in the X-linked and autosomal dominant forms of this syndrome, ..
  57. Chen G, Wang J, Liu Z, Kornmann M. Exon III splicing of fibroblast growth factor receptor 1 is modulated by growth factors and cyclin D1. Pancreas. 2008;37:159-64 pubmed publisher
    b>Fibroblast growth factor receptor 1 (FGFR1) isoform IIIc enhances and FGFR1-IIIb inhibits pancreatic cancer cell growth. Nothing is presently known about the expression and regulation of human FGFR1-III isoforms...
  58. Elbauomy Elsheikh S, Green A, Lambros M, Turner N, Grainge M, Powe D, et al. FGFR1 amplification in breast carcinomas: a chromogenic in situ hybridisation analysis. Breast Cancer Res. 2007;9:R23 pubmed
    ..The second core encompasses important oncogene candidates, including the fibroblast growth factor receptor 1 (FGFR1) gene...
  59. Raivio T, Sidis Y, Plummer L, Chen H, Ma J, Mukherjee A, et al. Impaired fibroblast growth factor receptor 1 signaling as a cause of normosmic idiopathic hypogonadotropic hypogonadism. J Clin Endocrinol Metab. 2009;94:4380-90 pubmed publisher
    b>FGFR1 mutations have been identified in about 10% of patients with Kallmann syndrome. Recently cases of idiopathic hypogonadotropic hypogonadism (IHH) with a normal sense of smell (nIHH) have been reported...
  60. Craddock K, Ludkovski O, Sykes J, Shepherd F, Tsao M. Prognostic value of fibroblast growth factor receptor 1 gene locus amplification in resected lung squamous cell carcinoma. J Thorac Oncol. 2013;8:1371-7 pubmed publisher
    b>Fibroblast growth factor receptor 1 (FGFR1) gene amplification was recently reported as a recurrent abnormality in 10% to 20% of primary lung squamous cell carcinomas (SqCCs), and has attracted significant interest as a potential ..
  61. Johnson D, Williams L. Structural and functional diversity in the FGF receptor multigene family. Adv Cancer Res. 1993;60:1-41 pubmed
  62. Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh B, et al. Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science. 1997;276:955-60 pubmed
    ..Two compounds from this class inhibited the kinase activity of fibroblast growth factor receptor 1 (FGFR1) and showed differential specificity toward other receptor tyrosine kinases...
  63. Carpenter G, Ji Q. Phospholipase C-gamma as a signal-transducing element. Exp Cell Res. 1999;253:15-24 pubmed
    ..However, the biochemistry of PLC-gamma is at a more advanced state than a clear understanding of exactly how this signaling element functions in the generation of a mitogenic response. ..
  64. Stachowiak E, Fang X, Myers J, Dunham S, Stachowiak M. cAMP-induced differentiation of human neuronal progenitor cells is mediated by nuclear fibroblast growth factor receptor-1 (FGFR1). J Neurochem. 2003;84:1296-312 pubmed
    ..We show that nuclear fibroblast growth factor receptor-1 (FGFR1) mediates cAMP-induced neuronal differentiation and regulates CREB and CREB binding protein (CBP) function in ..
  65. Heist R, Mino Kenudson M, Sequist L, Tammireddy S, Morrissey L, Christiani D, et al. FGFR1 amplification in squamous cell carcinoma of the lung. J Thorac Oncol. 2012;7:1775-1780 pubmed publisher
    Amplification of fibroblast growth factor receptor 1 (FGFR1) has been reported in squamous cell lung carcinoma and may be a molecular target for therapy...
  66. Lundin L, Ronnstrand L, Cross M, Hellberg C, Lindahl U, Claesson Welsh L. Differential tyrosine phosphorylation of fibroblast growth factor (FGF) receptor-1 and receptor proximal signal transduction in response to FGF-2 and heparin. Exp Cell Res. 2003;287:190-8 pubmed
    ..Our data imply that tyrosine 463 is phosphorylated and able to transduce signals in response to FGF-2 treatment alone; furthermore, we suggest that FGFR-1 dimerization/kinase activation is stabilized by heparin. ..
  67. Zhang J, Zhang L, Su X, Li M, Xie L, Malchers F, et al. Translating the therapeutic potential of AZD4547 in FGFR1-amplified non-small cell lung cancer through the use of patient-derived tumor xenograft models. Clin Cancer Res. 2012;18:6658-67 pubmed publisher
    To investigate the incidence of FGFR1 amplification in Chinese non-small cell lung cancer (NSCLC) and to preclinically test the hypothesis that the novel, potent, and selective fibroblast growth factor receptor (FGFR) small-molecule ..
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    ..Although amplification of HER2, C-MYC, CCND1 and FGFR1 has been reported in breast cancers, their role in the progression of in situ to invasive breast carcinoma is ..
  69. Reis Filho J, Simpson P, Turner N, Lambros M, Jones C, Mackay A, et al. FGFR1 emerges as a potential therapeutic target for lobular breast carcinomas. Clin Cancer Res. 2006;12:6652-62 pubmed
    ..However, little is known about the putative therapeutic targets for these tumors. The aim of this study was to characterize CLCs at the molecular genetic level and identify putative therapeutic targets...
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    b>Fibroblast growth factor receptor 1 (FGFR1) is a transmembrane protein capable of transducing stimulation by secreted FGFs...
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    Amplification of fibroblast growth factor receptor 1 (FGFR1) occurs in approximately 10% of breast cancers and is associated with poor prognosis...
  72. Chioni A, Grose R. FGFR1 cleavage and nuclear translocation regulates breast cancer cell behavior. J Cell Biol. 2012;197:801-17 pubmed publisher
    FGF-10 and its receptors, FGFR1 and FGFR2, have been implicated in breast cancer susceptibility and progression, suggesting that fibroblast growth factor (FGF) signaling may be co-opted by breast cancer cells...
  73. Göke F, Franzen A, Menon R, Goltz D, Kirsten R, Boehm D, et al. Rationale for treatment of metastatic squamous cell carcinoma of the lung using fibroblast growth factor receptor inhibitors. Chest. 2012;142:1020-1026 pubmed publisher
    We previously identified amplification of the fibroblast growth factor receptor 1 gene (FGFR1) as a potential therapeutic target for small-molecule inhibitor therapy in squamous cell lung cancer (L-SCC)...
  74. Haugsten E, Sørensen V, Brech A, Olsnes S, Wesche J. Different intracellular trafficking of FGF1 endocytosed by the four homologous FGF receptors. J Cell Sci. 2005;118:3869-81 pubmed
    ..For this purpose, we transfected HeLa cells with any one of the four tyrosine kinase FGF receptors (FGFR1-4)...
  75. Zou L, Cao S, Kang N, Huebert R, Shah V. Fibronectin induces endothelial cell migration through ?1 integrin and Src-dependent phosphorylation of fibroblast growth factor receptor-1 at tyrosines 653/654 and 766. J Biol Chem. 2012;287:7190-202 pubmed publisher
    ..that the provisional matrix protein, fibronectin (FN), activates fibroblast growth factor (FGF) receptor-1 (FGFR1) independent of FGF ligand in liver endothelial cells...
  76. Sasaki H, Shitara M, Yokota K, Hikosaka Y, Moriyama S, Yano M, et al. Increased FGFR1 copy number in lung squamous cell carcinomas. Mol Med Rep. 2012;5:725-8 pubmed publisher
    The basic fibroblast growth factor (bFGF), via activation of its receptor, FGFR1, has been postulated to be an important inducer of host stromal response and angiogenesis...
  77. Zhang X, Ibrahimi O, Olsen S, Umemori H, Mohammadi M, Ornitz D. Receptor specificity of the fibroblast growth factor family. The complete mammalian FGF family. J Biol Chem. 2006;281:15694-700 pubmed
    ..This study completes the mitogenesis-based comparison of receptor specificity of the entire FGF family under standard conditions and should help in interpreting and predicting in vivo biological activity. ..
  78. Pitteloud N, Acierno J, Meysing A, Eliseenkova A, Ma J, Ibrahimi O, et al. Mutations in fibroblast growth factor receptor 1 cause both Kallmann syndrome and normosmic idiopathic hypogonadotropic hypogonadism. Proc Natl Acad Sci U S A. 2006;103:6281-6 pubmed
    Mutations in KAL1 and FGFR1 cause Kallmann syndrome (KS), whereas mutations in the GNRHR and GPR54 genes cause idiopathic hypogonadotropic hypogonadism with normal olfaction (nIHH)...
  79. Bade L, Goldberg J, Dehut H, Hall M, Schwertfeger K. Mammary tumorigenesis induced by fibroblast growth factor receptor 1 requires activation of the epidermal growth factor receptor. J Cell Sci. 2011;124:3106-17 pubmed publisher
    b>Fibroblast growth factor receptor 1 (FGFR1) is an oncoprotein with known involvement in mammary tumorigenesis. To understand how FGFR1 signaling promotes mammary tumorigenesis, an inducible FGFR1 (iFGFR1) system was created previously...
  80. Haugsten E, Malecki J, Bjørklund S, Olsnes S, Wesche J. Ubiquitination of fibroblast growth factor receptor 1 is required for its intracellular sorting but not for its endocytosis. Mol Biol Cell. 2008;19:3390-403 pubmed publisher
    ..in internalization and sorting of fibroblast growth factor receptor (FGFR), we constructed several mutants of FGFR1 in which lysines, potential ubiquitination sites, were substituted for arginines...