PDGFs and their receptors

Gene. 2017 May 30:614:1-7. doi: 10.1016/j.gene.2017.03.003. Epub 2017 Mar 4.

Abstract

The platelet-derived growth factor (PDGF)/PDGFR receptor (PDGFR) family is essential for a vast array of physiological processes such as migration and proliferation of percityes that contribute to the formation and proper function of blood vessels. While ligand-dependent de-repression of the PDGFR's kinase activity is the major mode by which the PDGFR is activated, there are additional mechanisms to activate PDGFRs. Deregulated PDGFR activity contributes to various pathological conditions, and hence the PDGF/PDGFR family members are viable therapeutic targets. An increased appreciation of which PDGFR contributes to pathology, biomarkers that indicate the amplitude and mode of activation, and receptor-specific antagonists are necessary for the development of next-generation therapies that target the PDGF/PDGFR family.

Keywords: Activation of receptor tyrosine kinases; Indirect activation of PDGFR; Non-PDGFs; PDGF; PDGFR.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Molecular Targeted Therapy / methods
  • Multigene Family*
  • Neoplasms / drug therapy
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Platelet-Derived Growth Factor / antagonists & inhibitors
  • Platelet-Derived Growth Factor / genetics*
  • Platelet-Derived Growth Factor / metabolism
  • Protein Isoforms / antagonists & inhibitors
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism
  • Protein Kinase Inhibitors / therapeutic use
  • Receptors, Platelet-Derived Growth Factor / antagonists & inhibitors
  • Receptors, Platelet-Derived Growth Factor / genetics*
  • Receptors, Platelet-Derived Growth Factor / metabolism
  • Signal Transduction / drug effects
  • Signal Transduction / genetics*

Substances

  • Platelet-Derived Growth Factor
  • Protein Isoforms
  • Protein Kinase Inhibitors
  • Receptors, Platelet-Derived Growth Factor