Platelet-derived growth factor receptor alpha (PDGFR-α) and Platelet-derived growth factor receptor beta (PDGFR-β) (PDGFR-α/β)

Platelet-derived growth factor receptors (PDGFR-α and PDGFR-β) are essential cell surface receptor tyrosine kinases that mediate signals for cell survival, proliferation, and chemotaxis (UniProt P16234, P09619). These receptors are activated upon binding to PDGF ligands, leading to dimerization and autophosphorylation of their intracellular domains, which subsequently triggers downstream signaling pathways like PI3K/AKT and MAPK (PubMed: 15121856). While they are vital for normal mesenchymal cell development and wound repair, their aberrant activation is a hallmark of several pathological conditions (StatPearls: NBK539791). In oncology, mutations or gene fusions involving PDGFRA or PDGFRB drive the progression of gastrointestinal stromal tumors (GIST), certain leukemias, and gliomas (NIH: PDQ Cancer Information). Consequently, they are primary targets for multi-kinase inhibitors such as imatinib and sunitinib, which aim to disrupt the oncogenic signaling cascades (DrugBank: DB00619).

Other names

PDGFRAPDGFRBCD140aCD140bPlatelet-derived growth factor receptor 1Platelet-derived growth factor receptor 2PDGFR-1PDGFR-2Alpha-type platelet-derived growth factor receptorBeta-type platelet-derived growth factor receptor

Small molecule inhibition of the intracellular tyrosine kinase domain by competing with ATP binding (e.g., Imatinib), or monoclonal antibody-mediated blockade of the extracellular ligand-binding domain (e.g., Olaratumab) (PubMed: 28341595).