PDGFR
PDGFR stands for platelet-derived growth factor receptor, a pair of transmembrane receptor tyrosine kinases consisting of PDGFR-α and PDGFR-β. They are activated by binding of PDGFs (PDGF-A, -B, -C, -D) and form homo- or heterodimers, which triggers trans-autophosphorylation and activation of downstream signaling.
The receptors have an extracellular ligand-binding domain with immunoglobulin-like loops, a single-pass transmembrane helix, and an
PDGF ligands form dimers; PDGF-AA binds PDGFR-α; PDGF-BB binds PDGFR-β; PDGF-CC binds PDGFR-α and PDGF-DD binds PDGFR-β.
Activated PDGFRs stimulate signaling pathways including PI3K-Akt, Ras-MAPK, PLCγ, and STAT, promoting cell proliferation, survival, migration,
Pathologically, PDGFR signaling is implicated in cancers, gliomas, and fibrotic diseases. A hallmark in dermatofibrosarcoma protuberans
Therapeutically, PDGFR signaling is targeted by tyrosine kinase inhibitors such as imatinib, sunitinib, pazopanib, and sorafenib,