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FGFR1-3, VEGFR1-3, PDGFRα
- Target
- FGFR1-3, VEGFR1-3, PDGFRα
- Molecular classification
- Receptor tyrosine kinase (RTK), Receptor
01
Overview
Fibroblast growth factor receptors (FGFR1-3), vascular endothelial growth factor receptors (VEGFR1-3), and platelet-derived growth factor receptor alpha (PDGFRα) are families of receptor tyrosine kinases critically involved in cellular growth, differentiation, survival, migration, and angiogenesis. Their dysregulation is implicated in tumor progression, metastasis, and resistance to therapy across many cancer types. They are common therapeutic targets for small-molecule inhibitors and monoclonal antibodies aiming to inhibit tumor angiogenesis and disrupt aberrant growth factor signaling.
- Other names
- CD331 (FGFR1)CD332 (FGFR2)CD333 (FGFR3)FLT1 (VEGFR1)KDR/FLK1 (VEGFR2)FLT4 (VEGFR3)CD140a
02
Mechanism of action
Inhibition of tyrosine kinase activity: Small molecules or antibodies block ATP binding or dimerization, thereby blocking signal transduction. Blockade of ligand-binding: Prevent receptor activation by preventing ligand-receptor interaction. Downregulation of angiogenesis: Decreases tumor blood supply, inhibits growth and metastasis.
03
Biological functions
Signal transductionCell proliferationAngiogenesisCell survivalCell migrationTissue development and repair
04
Disease associations
CancerCardiovascular diseaseInflammatory diseasesFibrotic disordersDevelopmental disorders
05
Safety considerations
Off-target effectsHypertensionProteinuriaPoor wound healingHand-foot syndromeGastrointestinal effectsRisk of bleeding and thromboembolic eventsCardiac toxicityResistance mechanisms
06
Interacting drugs
Ponatinib
10 more in the full profile.
07
Biomarkers
FGFR mutations or fusions (especially in cancer, e.g., bladder, cholangiocarcinoma)VEGF/VEGFR expression levelsPDGF/PDGFRα amplification/mutation statuses
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