Obatoclax, saliphenylhalamide, and gemcitabine inhibit influenza a virus infection

J Biol Chem. 2012 Oct 12;287(42):35324-35332. doi: 10.1074/jbc.M112.392142. Epub 2012 Aug 21.

Abstract

Influenza A viruses (IAVs) infect humans and cause significant morbidity and mortality. Different treatment options have been developed; however, these were insufficient during recent IAV outbreaks. Here, we conducted a targeted chemical screen in human nonmalignant cells to validate known and search for novel host-directed antivirals. The screen validated saliphenylhalamide (SaliPhe) and identified two novel anti-IAV agents, obatoclax and gemcitabine. Further experiments demonstrated that Mcl-1 (target of obatoclax) provides a novel host target for IAV treatment. Moreover, we showed that obatoclax and SaliPhe inhibited IAV uptake and gemcitabine suppressed viral RNA transcription and replication. These compounds possess broad spectrum antiviral activity, although their antiviral efficacies were virus-, cell type-, and species-specific. Altogether, our results suggest that phase II obatoclax, investigational SaliPhe, and FDA/EMEA-approved gemcitabine represent potent antiviral agents.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / pharmacology*
  • Animals
  • Antiviral Agents / pharmacology*
  • Chlorocebus aethiops
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / pharmacology
  • Dogs
  • Gemcitabine
  • Humans
  • Indoles
  • Influenza A Virus, H3N2 Subtype / drug effects*
  • Influenza A Virus, H3N2 Subtype / physiology*
  • Influenza, Human / drug therapy*
  • Influenza, Human / metabolism
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Pyrroles / pharmacology*
  • RNA, Viral / biosynthesis
  • Salicylates / pharmacology*
  • Vero Cells
  • Virus Replication

Substances

  • Amides
  • Antiviral Agents
  • Indoles
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Proto-Oncogene Proteins c-bcl-2
  • Pyrroles
  • RNA, Viral
  • Salicylates
  • saliphenylhalamide
  • Deoxycytidine
  • obatoclax
  • Gemcitabine