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VEGFR1, VEGFR2, VEGFR3, FGFR1, FGFR2, PDGFRα, PDGFRβ

Molecular classification
Receptor tyrosine kinase, Transmembrane glycoprotein, Growth factor receptor
01

Overview

The vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), fibroblast growth factor receptors (FGFR1, FGFR2), and platelet-derived growth factor receptors (PDGFRα, PDGFRβ) are members of the receptor tyrosine kinase family. These proteins are transmembrane glycoproteins essential for cellular signal transduction pathways that regulate physiological processes including angiogenesis, lymphangiogenesis, cell survival, migration, and differentiation[1][2][3][4]. Dysregulation of these receptors is associated with numerous diseases, especially cancer, cardiovascular disorders, and inflammation[6][7]. Drugs targeting these receptors act by blocking ligand-induced activation and downstream signaling, primarily used to inhibit tumor vascularization and growth.\n\nGrouped as listed, these targets collectively represent the major signaling pathways modulated in anti-angiogenic and anti-proliferative therapies in oncology and related fields[3][7].

Other names
Flt-1Fms-like tyrosine kinase 1KDRFlk-1Flt-4CD140aPDGFR-alphaCD140bPDGFR-beta
02

Mechanism of action

Competitive inhibition of ATP binding to kinase domain, ligand (VEGF, FGF, PDGF) blockade, prevention of downstream phosphorylation cascades (MAPK, PI3K pathways), reduced endothelial cell proliferation and migration, and inhibition of neovascularization in tumors and tissues.

03

Biological functions

Signal transductionAngiogenesisLymphangiogenesisCell proliferationCell migrationVascular permeabilityEmbryonic developmentImmune response
04

Disease associations

CancerCardiovascular diseaseInflammationNeurodegenerative diseaseOther pathological and physiological angiogenesis
05

Safety considerations

Off-target effects (due to broad specificity of TKIs)HypertensionImpaired wound healing and bleedingProteinuria and nephrotic syndromeCardiac toxicityResistance mechanisms in tumors (e.g., signaling bypass, mutations)Limited efficacy due to compensatory angiogenic pathways
06

Interacting drugs

Sunitinib

6 more in the full profile.

07

Biomarkers

Expression levels of VEGFRs/FGFRs/PDGFRs (in tumors or tissue)Phosphorylation status of downstream signaling proteins (e.g., MAPK, AKT)Soluble VEGFRs in plasmaResponse to TKI therapyVEGF, FGF, PDGF ligand levels

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