Platelet-derived growth factor receptor alpha; Platelet-derived growth factor receptor beta (PDGFRA; PDGFRB)

Platelet-derived growth factor receptor alpha and Platelet-derived growth factor receptor beta are cell-surface receptors with intrinsic tyrosine kinase activity, each encoded by separate genes. They bind PDGF isoforms (homodimers and heterodimers of PDGF-A, PDGF-B, PDGF-C, PDGF-D), causing receptor homo- or heterodimerization. Ligand binding leads to activation via transphosphorylation of intracellular tyrosines, initiating downstream signaling pathways that control cell proliferation, migration, and differentiation. Aberrant activation is implicated in cancer, fibrotic, and proliferative diseases. They are well-established therapeutic targets for tyrosine kinase inhibitors.

Other names

PDGF receptor alphaPDGFRAPDGF receptor betaPDGFRBPDGFR-αPDGFR-β

Tyrosine kinase inhibition: drugs bind to the receptor’s kinase domain, preventing autophosphorylation and signal transduction