Target intelligence / Profile preview

VEGFR & PDGFR

Target
VEGFR & PDGFR
Molecular classification
Receptor tyrosine kinase, Cell surface receptor, Type III receptor tyrosine kinase family
01

Overview

VEGFR and PDGFR are families of transmembrane receptor tyrosine kinases that play central roles in angiogenesis, lymphangiogenesis, cell proliferation, migration, and survival. VEGFRs (VEGFR1, VEGFR2, VEGFR3) primarily regulate the response to vascular endothelial growth factors, controlling endothelial cell function and blood vessel formation. PDGFRs (PDGFRα, PDGFRβ) respond to platelet-derived growth factors, influencing connective tissue, vascular smooth muscle, and fibroblast biology. Both families signal via ligand-induced dimerization, resulting in autophosphorylation and activation of intracellular signaling cascades such as PI3K/AKT and MAPK. Therapeutic targeting of these receptors is critical in cancer, fibrosis, and retinal vascular diseases, and pharmacologic inhibition has proven effective but presents challenges related to safety and patient selection. The term 'VEGFR & PDGFR' incorrectly combines two distinct receptor families; for structured databases, these should be treated as separate entities.

Other names
Kinase insert domain receptor (KDR)Fetal liver kinase 1 (Flk-1)VEGF receptorPDGFRαPDGFRβPlatelet-derived growth factor receptor alpha/beta
02

Mechanism of action

Receptor inhibition (blocking ATP binding of the kinase domain to prevent phosphorylation); Ligand binding inhibition (antibody-based inhibition of the VEGF ligand); Signal transduction blockade (prevention of downstream PI3K/AKT, MAPK, PLC-γ1 pathway activation); Dimerization inhibition (prevents autophosphorylation needed for receptor activation)

03

Biological functions

Signal transductionAngiogenesisCell proliferationCell migrationVascular permeabilityLymphangiogenesisTissue regenerationInflammation
04

Disease associations

CancerCardiovascular diseaseInflammationRetinal diseasesFibrosisOther vascular proliferative disorders
05

Safety considerations

HypertensionProteinuriaBleeding riskThrombosis riskImpaired wound healingCardiac toxicityGastrointestinal perforationOther off-target toxicities associated with anti-angiogenic therapy
06

Interacting drugs

Bevacizumab

8 more in the full profile.

07

Biomarkers

VEGF-A levelsVEGF-C levelsVEGF-D levelsPDGF-AA levelsPDGF-BB levelsPhosphorylation status of VEGFR2 (e.g., Y1175, Y1214)Phosphorylation status of PDGFRβMicrovessel densityMutation status

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