Orphan nuclear receptor ERRγ is a key regulator of human fibrinogen gene expression

PLoS One. 2017 Jul 27;12(7):e0182141. doi: 10.1371/journal.pone.0182141. eCollection 2017.

Abstract

Fibrinogen, 1 of 13 coagulation factors responsible for normal blood clotting, is synthesized by hepatocytes. Detailed roles of the orphan nuclear receptors regulating fibrinogen gene expression have not yet been fully elucidated. Here, we identified estrogen-related receptor gamma (ERRγ) as a novel transcriptional regulator of human fibrinogen gene expression. Overexpression of ERRγ specially increased fibrinogen expression in human hepatoma cell line. Cannabinoid receptor types 1(CB1R) agonist arachidonyl-2'-chloroethylamide (ACEA) up-regulated transcription of fibrinogen via induction of ERRγ, whereas knockdown of ERRγ attenuated fibrinogen expression. Deletion analyses of the fibrinogen γ (FGG) gene promoter and ChIP assays revealed binding sites of ERRγ on human fibrinogen γ gene promoter. Moreover, overexpression of ERRγ was sufficient to increase fibrinogen gene expression, whereas treatment with GSK5182, a selective inverse agonist of ERRγ led to its attenuation in cell culture. Finally, fibrinogen and ERRγ gene expression were elevated in liver tissue of obese patients suggesting a conservation of this mechanism. Overall, this study elucidates a molecular mechanism linking CB1R signaling, ERRγ expression and fibrinogen gene transcription. GSK5182 may have therapeutic potential to treat hyperfibrinogenemia.

MeSH terms

  • Adult
  • Aged
  • Animals
  • Fibrinogen / genetics*
  • Fibrinogen / metabolism
  • Gene Expression Regulation*
  • Gene Knockdown Techniques
  • Hep G2 Cells
  • Humans
  • Liver / metabolism
  • Mice
  • Middle Aged
  • Non-alcoholic Fatty Liver Disease / genetics
  • Obesity / genetics
  • Promoter Regions, Genetic / genetics
  • Receptor, Cannabinoid, CB1 / metabolism
  • Receptors, Estrogen / metabolism*
  • Transcription, Genetic

Substances

  • ESRRG protein, human
  • Receptor, Cannabinoid, CB1
  • Receptors, Estrogen
  • Fibrinogen

Grants and funding

This work was supported by National Creative Research Initiatives Grant (20110018305) through the National Research Foundation of Korea (NRF) funded by the Korean government (Ministry of Science, ICT, & Future Planning); and Federal Ministry of Education and Research grant LiSyM (S.D., Grant PTJ-FKZ: 031L0043). B.D. was supported by a German Egyptian Research Long-Term Scholarship of DAAD/Egypt government.