PDGFRα/β heterodimer activation negatively affects downstream ERK1/2 signaling and cellular proliferation

Nat Commun. 2025 May 22;16(1):4754. doi: 10.1038/s41467-025-59938-1.

Abstract

The platelet-derived growth factor receptor (PDGFR) family of receptor tyrosine kinases consists of two receptors, PDGFRα and PDGFRβ, that homodimerize and heterodimerize upon ligand binding. Here, we tested the hypothesis that differential internalization and trafficking dynamics of the various PDGFR dimers underlie differences in downstream intracellular signaling and cellular behavior. Using a bimolecular fluorescence complementation approach, we demonstrated that PDGFRα/β heterodimers are rapidly internalized into early endosomes. We showed that PDGFRα/β heterodimer activation does not induce downstream phosphorylation of ERK1/2 and significantly inhibits cell proliferation. Further, we identified MYO1D as a protein that preferentially binds PDGFRα/β heterodimers and demonstrated that knockdown of MYO1D leads to retention of PDGFRα/β heterodimers at the plasma membrane, increased phosphorylation of ERK1/2 and increased cell proliferation. Collectively, our findings impart valuable insight into the molecular mechanisms by which specificity is introduced downstream of PDGFR activation to differentially propagate signaling and generate distinct cellular responses.

MeSH terms

  • Animals
  • Cell Membrane / metabolism
  • Cell Proliferation*
  • Endosomes / metabolism
  • HEK293 Cells
  • Humans
  • MAP Kinase Signaling System*
  • Mitogen-Activated Protein Kinase 1 / metabolism
  • Mitogen-Activated Protein Kinase 3* / metabolism
  • Phosphorylation
  • Protein Multimerization
  • Receptor, Platelet-Derived Growth Factor alpha* / genetics
  • Receptor, Platelet-Derived Growth Factor alpha* / metabolism
  • Receptor, Platelet-Derived Growth Factor beta* / genetics
  • Receptor, Platelet-Derived Growth Factor beta* / metabolism
  • Signal Transduction

Substances

  • Receptor, Platelet-Derived Growth Factor beta
  • Receptor, Platelet-Derived Growth Factor alpha
  • Mitogen-Activated Protein Kinase 3
  • Mitogen-Activated Protein Kinase 1
  • PDGFRB protein, human