FGFR1


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FGFR1

A gene on chromosome 8p12 that encodes fibroblast growth factor receptor-1, which has an extracellular region composed of 3 immunoglobulin-like domains, a single hydrophobic membrane-spanning segment and a cytoplasmic tyrosine kinase domain. Binding of a ligand unleashes a cascade of downstream signals that impact on mitogenesis and differentiation.

Molecular pathology
FGFR1 mutations are associated with inherited syndromes (e.g., Antley-Bixler syndrome, autosomal dominant Kallmann syndrome 2, Jackson-Weiss syndrome, osteoglophonic dysplasia and Pfeiffer syndrome), as well as myeloproliferative disorders and stem cell leukaemia lymphoma syndrome.
References in periodicals archive ?
Protein aliquots were separated on SDS-PAGE gels, transferred to PVDF membranes, blocked with 3% non-fat milk, and then incubated overnight with rabbit polyclonal antibodies against FGFR1 (sc-121, 1:400) and FGFR2 (sc-122, 1:600) (Santa Cruz Biotechnology, Santa Cruz, CA), respectively.
A number of drugs are in development that could stop the FGFR1 gene from working.
There are a number of drugs in development that stop FGFR1 working, and clinical studies are investigating whether these drugs work against cancers with too many copies of this gene.
showed that the inhibition of FGFR1 and FGFR2 increased cisplatin sensitivity in ovarian cancer (36).
Myeloid Neoplasms Associated with Eosinophilia and Abnormalities of PDGFRB and FGFR1.
Lenvatinib, discovered and developed by Eisai, is an oral molecular targeted agent that selectively inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors (VEGFR1 (FLT1), VEGFR2 (KDR) and VEGFR3 (FLT4)), in addition to other proangiogenic and oncogenic pathway-related RTKs (including fibroblast growth factor (FGF) receptors FGFR1, 2, 3 and 4; the platelet-derived growth factor (PDGF) receptor PDGFRalpha; KIT; and RET) involved in tumor proliferation.
Lenvatinib is an orally active, selective inhibitor of receptor tyrosine kinases (RTKs), including KDR (VEGFR-2), Flt-1 (VEGFR-1), FGFR1, PDGFR-?
14,15) Amplification of the FGFR1 and PI3k genes is found in about 20% and 8% of cases, respectively; mutations of DDR2 and FGFR3 are found in 3% and 1% of cases, respectively.
For example, many individuals with Pfeiffer syndrome have a common mutation in FGFR1 (1), which likely explains our failure to find a mutation in our one Pfeiffer case.
32) High-throughput capillary sequencing of 623 genes in 188 lung adenocarcinomas has identified several key pathways involved in lung cancer, as well as some potentially actionable driver mutations in ERBB3, ERBB4, FGFR1, FGFR2, FGFR4, and KDR.
LENVIMA also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFR[eth]), KIT, and RET.
Lenvatinib, discovered and developed by Eisai, is an orally active, selective inhibitor of receptor tyrosine kinases (RTKs) with a novel binding mode, including KDR (VEGFR-2), Flt-1 (VEGFR-1), RET, FGFR1, PDGFR-Beta and c-kit, involved in angiogenesis and tumor proliferation.