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Target intelligence / Profile preview
Platelet-derived growth factor alpha receptor (PDGFRα)
- Target
- PDGFRα
- Molecular classification
- Receptor, Receptor Tyrosine Kinase (RTK)
01
Overview
Platelet-derived growth factor alpha receptor (PDGFRα), also known as CD140a, is a cell surface receptor that plays a critical role in cellular signaling, development, and disease. Upon ligand binding (PDGF-A, -B, or -C), PDGFRα dimerizes, leading to autophosphorylation and activation of downstream signaling pathways involved in cell proliferation, survival, migration, and differentiation. Aberrant activation or mutations in PDGFRA are implicated in various neoplasms, including GISTs and other cancers.
- Other names
- CD140a
02
Mechanism of action
Tyrosine kinase inhibition via blocking ATP binding or receptor dimerization, leading to reduced downstream signaling.
03
Biological functions
Cell proliferationCell differentiationCell survivalEmbryonic developmentAngiogenesisSignal transduction
04
Disease associations
CancerGastrointestinal stromal tumors (GISTs)Clonal hypereosinophilia malignanciesGliomasSarcomasLeukemias
05
Safety considerations
Potential for off-target effects due to kinase inhibitor promiscuity.Development of resistance mutations.
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