Target intelligence / Profile preview

Vascular endothelial growth factor receptor family (VEGFR)

Target
VEGFR
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

The Vascular Endothelial Growth Factor Receptor (VEGFR) family consists of three primary receptor tyrosine kinases—VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4)—that play critical roles in the regulation of angiogenesis, vasculogenesis, and lymphangiogenesis (Source: UniProt P17948, P35968, P35916). These receptors are activated by the binding of VEGF ligands, leading to receptor dimerization and autophosphorylation of the intracellular tyrosine kinase domain, which triggers downstream signaling pathways such as PI3K/Akt and MAPK/ERK (Source: PubMed PMID: 12604457). In many pathological conditions, particularly solid tumors, the VEGFR pathway is overexpressed or overactive, promoting the formation of new blood vessels that supply nutrients to the tumor and facilitate metastasis (Source: PubMed PMID: 15585858). Consequently, the VEGFR family is a major therapeutic target in oncology, with numerous small-molecule multi-kinase inhibitors and monoclonal antibodies designed to block its activity (Source: FDA Drug Labels). Beyond cancer, VEGFR signaling is also a target in ophthalmic diseases like age-related macular degeneration, where excessive vessel growth impairs vision (Source: PubMed PMID: 24633614). The input name was marked as incorrect because the inclusion of "and other receptor tyrosine kinases" makes the target definition overly broad and non-specific for a single canonical entry.

Other names
VEGF receptorsVEGFR1-3FLT1KDRFLT4Vascular endothelial growth factor receptor 1Vascular endothelial growth factor receptor 2Vascular endothelial growth factor receptor 3
02

Mechanism of action

Competitive inhibition of the ATP-binding site within the intracellular tyrosine kinase domain of the receptors, preventing autophosphorylation and subsequent activation of downstream signaling cascades like MAPK/ERK and PI3K/Akt (Source: PubMed PMID: 15585858, StatPearls NBK538503).

03

Biological functions

AngiogenesisVasculogenesisLymphangiogenesisCell proliferationSignal transduction
04

Disease associations

CancerAge-related macular degenerationDiabetic retinopathyPsoriasis
05

Safety considerations

HypertensionProteinuriaHemorrhageWound healing complicationsHand-foot skin reactionGastrointestinal perforation
06

Interacting drugs

Sunitinib

9 more in the full profile.

07

Biomarkers

VEGF-A levelsVEGFR2 expressionTreatment-induced hypertensionSoluble VEGFR2 (sVEGFR2)

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