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Vascular endothelial growth factor receptor; Fibroblast growth factor receptor; Platelet-derived growth factor receptor; (and other receptor tyrosine kinases) (VEGFR; FGFR; PDGFR)

Target
VEGFR; FGFR; PDGFR
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

VEGFRs, FGFRs, and PDGFRs are families of **receptor tyrosine kinases** with key roles in regulating cellular processes including proliferation, survival, migration, and angiogenesis. These receptors share a common structural organization with extracellular ligand-binding domains, a single transmembrane helix, and an intracellular tyrosine kinase domain responsible for signal transduction. Upon ligand binding (such as VEGF, FGF, or PDGF), these receptors dimerize and autophosphorylate, leading to activation of multiple downstream signaling cascades (MAPK, PI3K/AKT, PLCγ). Dysregulation or overactivation is implicated in cancer, promoting tumor growth and metastasis, as well as pathological angiogenesis. As such, they are validated and widely pursued therapeutic targets, particularly in oncology and diseases involving aberrant vasculature.

Other names
VEGF receptor (VEGFR)FGF receptor (FGFR)PDGF receptor (PDGFR)Receptor tyrosine kinase (RTK) family
02

Mechanism of action

Inhibition of receptor tyrosine kinase activity; Blockade of downstream signaling pathways (e.g., MAPK, PI3K/AKT); Suppression of angiogenesis through decreased VEGF, FGF, or PDGF signaling; Induction of tumor cell apoptosis; Inhibition of tumor cell and endothelial cell proliferation

03

Biological functions

Signal transductionCell proliferationAngiogenesis (formation of new blood vessels)Cell survivalCell migrationCell differentiationApoptosis (programmed cell death)
04

Disease associations

CancerCardiovascular diseaseInflammationMetastasisOther solid tumors
05

Safety considerations

HypertensionProteinuriaHemorrhageCardiovascular events (e.g., thromboembolism)Hand-foot skin reactionFatigueGastrointestinal toxicity
06

Interacting drugs

Sunitinib

6 more in the full profile.

07

Biomarkers

Phosphorylated VEGFR, FGFR, or PDGFRVEGF, FGF, or PDGF ligand levelsDownstream pathway activation (e.g., phospho-ERK, phospho-AKT)

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