Target intelligence / Profile preview

Platelet-derived growth factor receptor alpha (PDGFR-alpha) (PDGFRA)

Target
PDGFRA
Molecular classification
Receptor tyrosine kinase, Type III receptor tyrosine kinase family, Receptor
01

Overview

Platelet-derived growth factor receptor alpha (PDGFR-alpha) is a cell-surface receptor tyrosine kinase that plays a fundamental role in regulating cell growth, chemotaxis, and differentiation (UniProt P16234). In the central nervous system, PDGFR-alpha is a hallmark marker for oligodendrocyte progenitor cells (OPCs), where it mediates the effects of PDGF ligands to maintain the progenitor pool and guide migration to areas requiring myelination (PubMed: 28250744). The signaling pathway is a critical regulator of the transition from a proliferative progenitor state to a differentiated, myelin-producing oligodendrocyte, making it a key focus in multiple sclerosis research (PubMed: 30655344). Beyond its role in development, PDGFR-alpha is a well-characterized oncogene; gain-of-function mutations or gene amplifications are primary drivers in a subset of gastrointestinal stromal tumors (GIST) and glioblastomas (NCI). Therapeutic interventions include small-molecule inhibitors like imatinib and avapritinib, which target the kinase domain, and monoclonal antibodies like olaratumab designed to prevent ligand binding (PubChem). Dysregulation of this receptor is also associated with hypereosinophilic syndrome and various fibrotic conditions, highlighting its broad clinical relevance (StatPearls).

Other names
PDGFRACD140APDGFR2Platelet-derived growth factor receptor 2Alpha-type platelet-derived growth factor receptorPDGFR-alpha
02

Mechanism of action

Small molecule inhibition of the intracellular tyrosine kinase domain and monoclonal antibody-mediated inhibition of the extracellular ligand-binding domain.

03

Biological functions

Signal transductionCell proliferationCell differentiationCell migrationMyelination
04

Disease associations

CancerNeurodegenerative diseaseGastrointestinal stromal tumorMultiple sclerosisGliomaHypereosinophilic syndrome
05

Safety considerations

Fluid retention and peripheral edemaMyelosuppression (neutropenia, anemia)Gastrointestinal distressPotential cardiotoxicityIntracranial hemorrhage
06

Interacting drugs

7 more in the full profile.

07

Biomarkers

PDGFRA mutation status (e.g., D842V)PDGFRA gene amplificationPDGFRA protein expression levels

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