Platelet-derived growth factor receptor alpha and beta (PDGFRα and PDGFRβ)

Platelet-derived growth factor receptors alpha and beta are cell surface **receptor tyrosine kinases** that bind members of the platelet-derived growth factor family. There are two main isoforms—**alpha** (*encoded by the* PDGFRA *gene*) and **beta** (*encoded by the* PDGFRB *gene*)—each with distinct but overlapping ligand specificities. Upon binding their ligands (various dimeric forms of PDGF), these receptors dimerize to form αα, ββ, or αβ complexes. Dimerization leads to activation via transphosphorylation on intracellular tyrosines, triggering downstream signaling cascades that regulate cellular processes such as proliferation, differentiation, migration, survival, and embryonic development. Dysregulation through mutation or overexpression is implicated in a variety of diseases including cancers like gastrointestinal stromal tumor (*especially with activating mutations in* PDGFRA), gliomas, leukemias as well as fibrotic disorders. These receptors are established therapeutic targets for several small-molecule kinase inhibitors used clinically.

Other names

PDGF receptor alpha (PDGFRα)PDGF receptor beta (PDGFRβ)CD140a (for alpha)CD140b (for beta)Platelet-derived growth factor receptorReceptor tyrosine kinase PDGFRA/PDGFRB

Inhibition of tyrosine kinase activity to block downstream signaling pathways involved in cell proliferation and survival.