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Fgfr1

Official Full Name
fibroblast growth factor receptor 1
Background
Fibroblast growth factor receptor 1 (FGFR1), also known as basic fibroblast growth factor receptor 1, fms-related tyrosine kinase-2 / Pfeiffer syndrome, and CD331, is a receptor tyrosine kinase whose ligands are specific members of the fibroblast growth factor family. FGFR1 has been shown to be associated with Pfeiffer syndrome.
Synonyms
FLG; FGFR1; fibroblast growth factor receptor 1; CEK; OGD; FLT2; KAL2; BFGFR; CD331; FGFBR; FLT-2; HBGFR; N-SAM; FGFR-1; FLJ99988; bFGF-R-1; OTTHUMP00000190874; OTTHUMP00000190875; OTTHUMP00000190876; OTTHUMP00000190877; OTTHUMP00000190879; OTTHUMP00000190880; OTTHUMP00000190881; OTTHUMP00000190885; proto-oncogene c-Fgr; FMS-like tyrosine kinase 2; hydroxyaryl-protein kinase; fms-related tyrosine kinase 2; heparin-binding growth factor receptor; H2; H3; H4; H5; Basic fibroblast growth factor receptor 1; N sam tyrosine kinase; Protein tyrosine kinase; Tyrosylprotein kinase; Hydroxyaryl protein kinase; Heparin binding growth factor receptor; FLT2, fms related tyrosine kinase 2 , KAL2; N SAM; Pfeiffer syndrome; FGFR1/PLAG1 fusion; cek1 protein; tyrosine kinase receptor CEK1

Cat.No. Product Name Price
AD06229ZHuman FGFR1 adenoviral particlesInquiry
Cat.No. Product Name Price
CDCB156572Cynomolgus FGFR1 ORF cloneInquiry
CDCB167477Chicken FGFR1 ORF Clone (NM_205510)Inquiry
CDCB186753Rabbit FGFR1 ORF clone (XM_008273979.1)Inquiry
CDCL108139Mouse FGFR1 ORF clone (NM_001174067.1)Inquiry
CDCL108141Mouse Fgfr1 ORF clone (NM_001079909.1)Inquiry
CDCL108159Mouse FGFR1 ORF clone (NM_015850.3)Inquiry
CDCL108161Human FGFR1 ORF clone (NM_023105.2)Inquiry
CDCL108165Mouse FGFR1 ORF clone (NM_001174064.1)Inquiry
CDCL184268Human FGFR1 ORF clone(NM_023106.2)Inquiry
CDCR234056Mouse Fgfr1 ORF Clone(NM_001079908.1)Inquiry
CDCR248627Mouse Fgfr1 ORF Clone(NM_010206.2)Inquiry
CDCR308469Human FGFR1 ORF Clone(NM_023110.2)Inquiry
CDCR356898Human FGFR1 ORF Clone(NM_001174063.1)Inquiry
CDCR356901Human FGFR1 ORF Clone(NM_001174065.1)Inquiry
CDCR356904Human FGFR1 ORF Clone(NM_001174066.1)Inquiry
CDCR379353Rat Fgfr1 ORF Clone(NM_024146.1)Inquiry
CDCS409053Human FGFR1 ORF Clone (BC015035)Inquiry
CDFG004105Human FGFR1 cDNA Clone(NM_023105.2)Inquiry
CDFG004111Human FGFR1 cDNA Clone(NM_023110.2)Inquiry
CDFG004113Human FGFR1 cDNA Clone(NM_023110.2)Inquiry
CDFH006842Human FGFR1 cDNA Clone(NM_001174063.1)Inquiry
CDFH006843Human FGFR1 cDNA Clone(NM_001174064.1)Inquiry
CDFH006844Human FGFR1 cDNA Clone(NM_001174065.1)Inquiry
CDFH006845Human FGFR1 cDNA Clone(NM_001174066.1)Inquiry
CDFH006846Human FGFR1 cDNA Clone(NM_001174067.1)Inquiry
CDFR012276Rat Fgfr1 cDNA Clone(NM_024146.1)Inquiry
MiUTR1H-03636FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1H-03637FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1H-03638FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1H-03639FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1H-03640FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1H-03641FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1H-03642FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1M-04702FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1M-04703FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1M-04704FGFR1 miRNA 3'UTR cloneInquiry
MiUTR1R-01899FGFR1 miRNA 3'UTR cloneInquiry

The fibroblast growth factor receptor type 1 gene (FGFR1) is one of the most commonly amplified genes in human cancer. The fibroblast growth factor receptor (FGFR) tyrosine kinase family is comprised of four kinases, FGFR1, 2, 3, and 4, that play important role in development, and have been shown to be targets for deregulation by either amplification, point mutation, or translocation. FGFRs, as members of the receptor tyrosine kinase (RTK) family, are known to signal, after ligand binding and receptor dimerization, from the cell membrane as well as from endosomal compartments. Signal transduction, primarily through the MAPK pathway but also acting via phosphoinositide 3-kinase (PI3K), STATs, and PLC-γ, leads to activation of several known target genes (e.g., CyclinD1 and PEA3) to modulate cell behavior. In addition to these well-studied signaling pathways, there is a growing body of evidence showing that full-length FGFRs, and FGFR1 in particular, can be targeted to the nucleus.

The FGFR signaling pathway is implicated in a wide range of pathologies, most notably cancer, yet its efficient targeting is proving challenging to the pharmaceutical industry, partly because FGFR signaling is fundamental to so many normal biological processes. More and more data has suggested that targeting FGFR1 might represent a novel therapeutic approach in blocking cancer invasion. Amplification or activation of FGFR1 has been reported in oral squamous carcinoma, esophageal squamous cell carcinomas, ovarian cancer, prostate cancer, bladder cancer, and lung cancer. Consistent with this, a pan-FGFR tyrosine kinase inhibitor has been shown to block tumor proliferation in a subset of non-small cell lung cancer (NSCLC) cell lines with activated FGFR signaling but has no effect on cells that do not activate the pathway. FGFR1 has been identified as the driver event in breast carcinomas and NSCLC, especially squamous cell lung carcinomas, harboring similar amplifications of the 8p11 chromosomal segment.

FGFR1 and lung cancer

A recent report identifies FGFR1 as a potential therapeutic target in NSCLC, where 8p11-12 amplification is common, suggesting that high levels of expression of FGFR1 may contribute to tumorigenesis or progression in NSCLC. As FGFR1 amplification has been reported in other tumor types, it may be the case that FGFR1 inhibition will be a successful therapeutic strategy in a variety of settings. Because some FGFR kinase inhibitors are now in clinical trials, including dovitinib, brivanib, BIBF 1120, and SU-6668, it could be useful to test these inhibitors on NSCLC patients bearing focal FGFR1 amplification. Given that amplification alone will not always predict sensitivity to FGFR1 inhibition, additional work is needed to fully characterize the genetic alterations involved in NSCLC carcinogenesis and dependency on FGFR1.

FGFR1 and breast cancer

Amplification of FGFR1 occurs in ∼10% of breast cancers and is associated with poor prognosis. Breast cancer cell lines with FGFR1 overexpression show enhanced ligand-dependent signaling, with increased activation of the mitogen-activated protein kinase and phosphoinositide 3-kinase–AKT signaling pathways in response to FGF2, but also show basal ligand-independent signaling, and are dependent on FGFR signaling for anchorage-independent growth. Moreover, some studies show that amplified cancers have a high proliferative rate assessed by Ki67 staining and that FGFR1 amplification is found in 16% to 27% of luminal B–type breast cancers. The amplification and overexpression of FGFR1 may be a major contributor to poor prognosis in luminal-type breast cancers, driving anchorage-independent proliferation and endocrine therapy resistance. In short, FGFR1 amplification is one of the major drivers of highly proliferative, poor-prognosis, luminal B subtype, ER-positive breast cancers. This provides a strong rationale for the investigation of drugs that target FGFR1 in breast cancer, particularly in combination with endocrine therapy.

References:

  1. Chioni A M, Grose R. FGFR1 cleavage and nuclear translocation regulates breast cancer cell behavior. J Cell Biol, 2012, 197(6): 801-817.
  2. Yang F, et al. FGFR1 Is Essential for Prostate Cancer Progression and Metastasis. Cancer Research, 2013, 73(12):3716-3724.
  3. Brewer J R, et al. Fgfr1 regulates development through the combinatorial use of signaling proteins. Genes & Development, 2015.
  4. Dutt A, et al. Inhibitor-Sensitive FGFR1 Amplification in Human Non- Small Cell Lung Cancer. PLoS ONE, 2011, 6(6):e20351.
  5. Turner N, et al. FGFR1 Amplification Drives Endocrine Therapy Resistance and Is a Therapeutic Target in Breast Cancer. Cancer Research, 2010, 70(5):2085-2094.

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