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Fibroblast Growth Factor Receptor 4 (FGFR4)
- Target
- FGFR4
- Molecular classification
- Receptor Tyrosine Kinase, Receptor
01
Overview
Fibroblast growth factor receptor 4 (FGFR4) is a receptor tyrosine kinase that belongs to the FGFR family. It plays a crucial role in cell proliferation, differentiation, migration, and metabolism. FGFR4 is activated by fibroblast growth factors (FGFs), leading to downstream signaling through MAPK/ERK and PI3K/AKT pathways. It is implicated in various cancers, including breast, ovarian, prostate, gastric, and pancreatic cancers, making it a therapeutic target. A common polymorphism, Gly388Arg, is associated with worse prognosis in several cancer types. Selective FGFR4 inhibitors are under development as cancer therapeutics.
- Other names
- CD334
02
Mechanism of action
Small molecule inhibitors selectively targeting the FGFR4 kinase domain, blocking its autophosphorylation and downstream signaling.
03
Biological functions
Cell proliferationCell differentiationCell migrationMetabolismSignal transductionAngiogenesisWound healingEmbryonic developmentMitogenesisNuclear gene regulation
04
Disease associations
CancerPituitary tumorsGastric cancerPancreatic cancer
05
Safety considerations
Potential for off-target effects with pan-FGFR inhibitors.Resistance development
06
Interacting drugs
BLU9931
1 more in the full profile.
07
Biomarkers
FGFR4 overexpressionFGFR4 amplificationGly388Arg (rs351855) polymorphism
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