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VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β, and c-Kit (Multiple RTKs)
- Target
- Multiple RTKs
- Molecular classification
- Receptor, Receptor tyrosine kinase, Growth factor receptor
01
Overview
This entry describes a group of important therapeutic targets, including VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β, and c-Kit, all of which are receptor tyrosine kinases. While distinct entities, they share roles in critical biological processes like angiogenesis, cell proliferation, migration, and survival, and are often co-targeted in cancer and vascular diseases. Inhibition of these targets, typically via multi-kinase inhibitors, can lead to significant safety concerns related to their broad biological impact. Each can be amenable to biomarker-guided therapy.
- Other names
- Flt-1FLT1KDRFlk-1FLT4PDGFRBKITCD117Stem cell factor receptor
02
Mechanism of action
Inhibition of tyrosine kinase activity and growth factor binding for receptor activation, blocking receptor activation
03
Biological functions
AngiogenesisSignal transductionCell proliferationVascular developmentEndothelial cell proliferationVascular permeabilityLymphangiogenesisMigrationSurvivalFibrosisHematopoiesisStem cell maintenanceGametogenesisMelanogenesis
04
Disease associations
CancerCardiovascular diseaseInflammationEye diseaseOcular neovascularizationLymphedemaInflammatory diseaseFibrosisGISTMelanomaLeukemiaAnemiaInfertilityPigmentary disorders
05
Safety considerations
HypertensionHemorrhageImpaired wound healingProteinuriaArterial thromboembolismEdemaLymphatic dysfunctionMyelosuppressionFluid retentionCardiotoxicityPigmentation changesInfertilityIncreased risk of infections
06
Interacting drugs
Bevacizumab
12 more in the full profile.
07
Biomarkers
VEGFR-1 expression (endothelial tissue)soluble VEGFR-1 (plasma)VEGFR-2 expression (tumor endothelium)phosphorylated VEGFR-2VEGFR-3 expression (lymphatic endothelium)phosphorylated VEGFR-3PDGFR-β expression (tumor stromal/cancer cells)phospho-PDGFR-βc-Kit mutation status (e.g., in GIST)c-Kit expression (IHC)
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