Protease activated receptor-1 deficiency diminishes bleomycin-induced skin fibrosis

Mol Med. 2014 Sep 18;20(1):410-6. doi: 10.2119/molmed.2014.00027.

Abstract

Accumulating evidence shows that protease-activated receptor-1 (PAR-1) plays an important role in the development of fibrosis, including lung fibrosis. However, whether PAR-1 also plays a role in the development of skin fibrosis remains elusive. The aim of this study was to determine the role of PAR-1 in the development of skin fibrosis. To explore possible mechanisms by which PAR-1 could play a role, human dermal fibroblasts and keratinocytes were stimulated with specific PAR-1 agonists or antagonists. To investigate the role of PAR-1 in skin fibrosis, we subjected wild-type and PAR-1-deficient mice to a model of bleomycin-induced skin fibrosis. PAR-1 activation leads to increased proliferation and extra cellular matrix (ECM) production, but not migration of human dermal fibroblasts (HDF) in vitro. Moreover, transforming growth factor (TGF)-β production was increased in keratinocytes upon PAR-1 activation, but not in HDF. The loss of PAR-1 in vivo significantly attenuated bleomycin-induced skin fibrosis. The bleomycin-induced increase in dermal thickness and ECM production was reduced significantly in PAR-1-deficient mice compared with wild-type mice. Moreover, TGF-β expression and the number of proliferating fibroblasts were reduced in PAR-1-deficient mice although the difference did not reach statistical significance. This study demonstrates that PAR-1 contributes to the development of skin fibrosis and we suggest that PAR-1 potentiates the fibrotic response mainly by inducing fibroblast proliferation and ECM production.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bleomycin
  • Cell Line
  • Cell Proliferation
  • Cells, Cultured
  • Extracellular Matrix / metabolism
  • Fibroblasts / metabolism
  • Fibroblasts / pathology*
  • Fibrosis
  • Humans
  • Keratinocytes / metabolism
  • Keratinocytes / pathology*
  • Male
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Receptor, PAR-1 / agonists
  • Receptor, PAR-1 / antagonists & inhibitors
  • Receptor, PAR-1 / genetics
  • Receptor, PAR-1 / metabolism*
  • Skin / drug effects
  • Skin / pathology*
  • Skin Diseases / chemically induced
  • Skin Diseases / metabolism*
  • Skin Diseases / pathology

Substances

  • Receptor, PAR-1
  • Bleomycin