Targeting of Discoidin Domain Receptor 2 (DDR2) Prevents Myofibroblast Activation and Neovessel Formation During Pulmonary Fibrosis

Mol Ther. 2016 Oct;24(10):1734-1744. doi: 10.1038/mt.2016.109. Epub 2016 May 27.

Abstract

Idiopathic pulmonary fibrosis (IPF) is a lethal human disease with short survival time and few treatment options. Herein, we demonstrated that discoidin domain receptor 2 (DDR2), a receptor tyrosine kinase that predominantly transduces signals from fibrillar collagens, plays a critical role in the induction of fibrosis and angiogenesis in the lung. In vitro cell studies showed that DDR2 can synergize the actions of both transforming growth factor (TGF)-β and fibrillar collagen to stimulate lung fibroblasts to undergo myofibroblastic changes and vascular endothelial growth factor (VEGF) expression. In addition, we confirmed that late treatment of the injured mice with specific siRNA against DDR2 or its kinase inhibitor exhibited therapeutic efficacy against lung fibrosis. Thus, this study not only elucidated novel mechanisms by which DDR2 controls the development of pulmonary fibrosis, but also provided candidate target for the intervention of this stubborn disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Differentiation
  • Cells, Cultured
  • Collagen Type I / metabolism
  • Discoidin Domain Receptor 2 / antagonists & inhibitors
  • Discoidin Domain Receptor 2 / metabolism*
  • Disease Models, Animal
  • Extracellular Matrix / metabolism*
  • Humans
  • Mice
  • Myofibroblasts / cytology*
  • Myofibroblasts / metabolism
  • Protein Kinase Inhibitors / administration & dosage
  • Protein Kinase Inhibitors / therapeutic use
  • Pulmonary Fibrosis / drug therapy
  • Pulmonary Fibrosis / metabolism*
  • RNA, Small Interfering / administration & dosage
  • RNA, Small Interfering / pharmacology
  • Transforming Growth Factor beta / metabolism
  • Up-Regulation
  • Vascular Endothelial Growth Factor A / metabolism*

Substances

  • Collagen Type I
  • Protein Kinase Inhibitors
  • RNA, Small Interfering
  • Transforming Growth Factor beta
  • VEGFA protein, human
  • Vascular Endothelial Growth Factor A
  • DDR2 protein, human
  • Discoidin Domain Receptor 2