The kinase inhibitor Sorafenib impairs the antiviral effect of interferon α on hepatitis C virus replication

Eur J Cell Biol. 2013 Jan;92(1):12-20. doi: 10.1016/j.ejcb.2012.09.001. Epub 2012 Oct 27.

Abstract

Recently, it was shown that the kinase inhibitor Sorafenib efficiently blocks HCV replication by inhibition of c-Raf. However, a longer treatment with higher doses of Sorafenib might be associated with adverse effects. Therefore, it was analysed whether a decreased dose of Sorafenib can be applied in combination with interferon α to obtain additive antiviral, but at the same time decreased adverse effects. However, Sorafenib abolishes the inhibitory effect of interferon α on HCV replication and vice versa. In order to reveal the underlying mechanisms, we observed that on the one hand IFNα activates c-Raf and thereby counteracts the inhibitory effect of Sorafenib on HCV replication that is based on the Sorafenib-dependent inhibition of c-Raf. On the other hand we found that the IFNα-induced PKR-phosphorylation depends on c-Raf. So, Sorafenib as a potent inhibitor of c-Raf prevents the IFNα-dependent PKR phosphorylation. Moreover, Sorafenib inhibits c-Raf-independent the phosphorylation of STAT1 resulting in an impaired induction of IFNα-dependent genes. Taken together, these data indicate that a combined application of Sorafenib and interferon α in order to obtain an antiviral effect is not useful since Sorafenib exerts an inhibitory effect on targets that are crucial for the transduction of interferon α-dependent antiviral response.

MeSH terms

  • Antiviral Agents / antagonists & inhibitors*
  • Cell Line, Tumor
  • Hepacivirus / physiology*
  • Humans
  • Interferon-alpha / antagonists & inhibitors*
  • Niacinamide / analogs & derivatives*
  • Niacinamide / pharmacology
  • Phenylurea Compounds / pharmacology*
  • Phosphorylation
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors
  • Sorafenib
  • Virus Replication / drug effects*

Substances

  • Antiviral Agents
  • Interferon-alpha
  • Phenylurea Compounds
  • Protein Kinase Inhibitors
  • Niacinamide
  • Sorafenib
  • Proto-Oncogene Proteins c-raf