FGFR4


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FGFR4

A gene on chromosome 5q35.1-qter that encodes fibroblast growth factor receptor-4, which has an extracellular region composed of 3 immunoglobulin-like domains, a single hydrophobic membrane-spanning segment and a cytoplasmic tyrosine kinase domain. The function of FGFR4 is unknown.

Molecular pathology
FGFR4 is overexpressed in gynaecological tumours, suggesting a role in breast and ovarian malignancies.
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It is well established that the signals evoked by FGF family members are converted by four major FGFRs, namely FGFR1 to FGFR4, to exert myriad biological effects on embryonic development and homeostasis in the adult for a wide range of tissues (14).
Elevated cholesterol metabolism and bile acid synthesis in mice lacking membrane tyrosine kinase receptor FGFR4.
Survival tree analysis revealed FGF2, FGFR2, FGFR4, FGF14, and FGF23 gene- gene interactions, indicating FGF2 rs167428 to be the primary factor contributing to overall survival.
Identification of FGFR4 as a potential therapeutic target for advanced-stage, high-grade serous ovarian cancer.
6] Human genes: FGF2, fibroblast growth factor 2 (basic); FGF1, fibroblast growth factor 1 (acidic); FGF7, fibroblast growth factor 7; FGFR1, fibroblast growth factor receptor1; FGF18, fibroblast growth factor 18; FGF23, fibroblast growth factor 23; FGF5, fibroblast growth factor 5; FGFR2, fibroblast growth factor receptor 2; FGFR4, fibroblast growth factor receptor 4; FGF14, fibroblast growth factor 14; FGF9, fibroblast growth factor 9; FGF10, fibroblast growth factor 10.
BLU-554 showed significant anti-tumor efficacy and was well-tolerated in two in vivo models of HCC driven by aberrant FGFR4 signaling, one with genomic amplification of FGFR4-activating ligand FGF19 and another with FGF19 overexpression in the absence of amplification.
Potent inhibition of FGFR4 and greater than 100-fold more selectivity for FGFR4 than FGFR1-3 in in vitro studies.
The Cancer Discovery publication outlines the unique discovery process led by Blueprint Medicines' scientists to craft selective, covalent drugs to FGFR4, which historically had been a challenging kinase for drug discovery due to the sequence similarities with the other FGFR paralogs.
Greater than fifty-fold selectivity for FGFR4 relative to other FGFR family members and little to no inhibition of all other kinases;
The proceeds from this financing provide us with the financial strength to initiate clinical trials for our FGFR4 and KIT Exon 17 inhibitors in 2015 with the goal of establishing proof of concept rapidly and ultimately improving the lives of patients," said Jeffrey Albers, chief executive officer of Blueprint Medicines.
BLU-554 is the first known selective FGFR4 inhibitor.
BLU-554: The first known paralog-selective FGFR4 inhibitor for patients suffering from hepatocellular carcinoma with FGFR4 pathway activation.