Target intelligence / Profile preview

Platelet-derived growth factor receptor; Vascular endothelial growth factor receptor; Transforming growth factor beta receptor; Insulin-like growth factor 1 receptor (PDGFR; VEGFR; TGF-β receptor (or TGFBR); IGF-1R)

Target
PDGFR; VEGFR; TGF-β receptor (or TGFBR); IGF-1R
Molecular classification
Receptor tyrosine kinases (RTKs), Growth factor receptor family, PDGFR (class III RTK), VEGFR (class V RTK), TGF-β receptor (serine/threonine kinase receptor, but with RTK-like features), IGF-1R (class II RTK)
01

Overview

These four targets—platelet-derived growth factor receptor (PDGFR), vascular endothelial growth factor receptor (VEGFR), transforming growth factor beta receptor (TGF-β receptor), and insulin-like growth factor 1 receptor (IGF-1R)—are functionally related receptor tyrosine kinases or serine/threonine kinase receptors that mediate growth factor signaling involved in cell proliferation, angiogenesis, survival, migration, and differentiation. They are well-established therapeutic targets in oncology, fibrotic diseases, and other proliferative disorders. Drugs targeting these pathways are either small-molecule kinase inhibitors or monoclonal antibodies that block ligand-receptor interactions. Their upregulation or mutation is closely associated with cancer and other pathologies, and their inhibition can also be associated with significant safety risks.

Other names
platelet-derived growth factor receptorCD140vascular endothelial growth factor receptorFLT1 (VEGFR-1)KDR/FLK1 (VEGFR-2)FLT4 (VEGFR-3)transforming growth factor beta receptorTGFBRI (ALK5)TGFBRIITGFBRIIIinsulin-like growth factor 1 receptorIGFIR
02

Mechanism of action

Inhibition of receptor tyrosine kinase activity (small molecule inhibitors); Ligand sequestration (e.g., anti-VEGF antibodies); Monoclonal antibodies blocking receptor-ligand interaction; Signaling blockade via antibody or kinase inhibition (for TGF-β receptor, inhibition of serine/threonine kinase domain).

03

Biological functions

Signal transductionCell proliferationCell survivalAngiogenesisDifferentiationMigrationApoptosis regulation
04

Disease associations

Cancer (growth, progression, metastasis)FibrosisCardiovascular diseaseInflammationDiabetic complicationsOther proliferative and vascular diseases
05

Safety considerations

HypertensionHemorrhageImpaired wound healingCardiovascular toxicityDysregulated glucose metabolismFibrosisImmunosuppressionMyelosuppressionOff-target kinase toxicity
06

Interacting drugs

17 more in the full profile.

07

Biomarkers

Receptor expression (IHC/FISH assays)Circulating ligand levels (VEGF, PDGF, TGF-β, IGF-1)Downstream signaling molecules (phosphorylated ERK, AKT, SMADs)

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