Target intelligence / Profile preview

Platelet-derived growth factor receptor alpha subunit

Molecular classification
Receptor, Receptor Tyrosine Kinase, Class III Receptor Tyrosine Kinase
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Overview

Platelet-derived growth factor receptor alpha (PDGFRα), also known as CD140a, is a cell surface receptor tyrosine kinase. It is a critical regulator of cellular growth, differentiation, and development, particularly in mesodermal tissues. PDGFRα plays essential roles during embryogenesis and in maintaining tissue homeostasis. Ligand binding (PDGF-A, -B, -C) induces receptor dimerization and autophosphorylation, activating downstream signaling pathways like PI3K/AKT and MAPK. Mutations in PDGFRA are linked to GISTs and clonal hypereosinophilic syndromes, making it a clinically relevant target for therapies like imatinib.

Other names
PDGFRαCD140a
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Mechanism of action

Tyrosine kinase inhibitor; inhibits the tyrosine kinase activity of PDGFRα, preventing receptor autophosphorylation and downstream signaling.

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Biological functions

Cell growthCell differentiationEmbryonic developmentTissue maintenanceSignal transductionCell proliferationCell migrationCell survival
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Disease associations

CancerGastrointestinal stromal tumors (GISTs)Clonal hypereosinophilic syndromesFibrotic diseasesAtherosclerosisNeoplasms involving mesenchymal origin
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Safety considerations

Aberrant proliferation leading to tumor formation if negative feedback mechanisms are disrupted.
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Interacting drugs

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