Target intelligence / Profile preview

Platelet-derived growth factor receptor, Transforming growth factor beta receptor, Vascular endothelial growth factor receptor, and Epidermal growth factor receptor (Group) (PDGFR/TGFBR/VEGFR/EGFR)

Target
PDGFR/TGFBR/VEGFR/EGFR
Molecular classification
Receptor, Enzyme, Receptor tyrosine kinase, Serine/threonine protein kinase receptor
01

Overview

This target entry represents a composite of four distinct receptor families: Platelet-derived growth factor receptor (PDGFR), Transforming growth factor beta receptor (TGFBR), Vascular endothelial growth factor receptor (VEGFR), and Epidermal growth factor receptor (EGFR). These receptors are critical mediators of cellular signaling, governing essential processes such as cell growth, survival, angiogenesis, and the epithelial-mesenchymal transition (EMT) (UniProt P00533, P17948, P09619, P36897). While PDGFR, VEGFR, and EGFR are members of the receptor tyrosine kinase (RTK) family, TGFBR functions as a serine/threonine kinase receptor. Dysregulation of these pathways is a hallmark of many malignancies and progressive fibrotic diseases, such as idiopathic pulmonary fibrosis and various solid tumors (PubMed: 28633859). Therapeutic strategies often utilize multi-kinase inhibitors, such as Nintedanib or Vandetanib, to simultaneously inhibit multiple pathways, thereby overcoming redundant signaling and drug resistance (StatPearls: NBK542279). This grouping is typically used in the context of broad-spectrum kinase inhibition targeting both the tumor microenvironment and the cancer cells themselves.

Other names
Receptor Tyrosine Kinases (RTKs)Growth Factor ReceptorsAngiokinase targetsFibrokinase targets
02

Mechanism of action

Inhibition of intracellular kinase domains (tyrosine or serine/threonine) to block ATP binding and prevent downstream signaling cascades such as MAPK/ERK, PI3K/Akt, and Smad pathways.

03

Biological functions

Signal transductionCell proliferationAngiogenesisEpithelial-mesenchymal transition (EMT)Wound healingCell survivalTissue remodeling
04

Disease associations

CancerFibrosisIdiopathic pulmonary fibrosisCardiovascular diseaseOcular neovascularization
05

Safety considerations

HypertensionHemorrhageGastrointestinal perforationDermatological toxicity (acneiform rash)DiarrheaImpaired wound healingInterstitial lung disease
06

Interacting drugs

Nintedanib

9 more in the full profile.

07

Biomarkers

EGFR mutation status (e.g., L858R, T790M)VEGF expression levelsPDGFR-beta expressionTGF-beta1 plasma levelsPhospho-Smad2/3 levels

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