An "All-In-One" Pharmacophoric Architecture for the Discovery of Potential Broad-Spectrum Anti-Flavivirus Drugs

Appl Biochem Biotechnol. 2018 Jul;185(3):799-814. doi: 10.1007/s12010-017-2690-2. Epub 2018 Jan 18.

Abstract

A precipitous increase in the number of flaviviral infections has been noted over the last 5 years. Despite these outbreaks, treatment protocols for infected individuals remain ambiguous. Numerous studies have identified NITD008 as a potent flavivirus inhibitor; however, clinical testing was dismissed due to undesirable toxic effects. The binding landscape of NITD008 in complex with five detrimental flaviviruses at the RNA-dependent RNA polymerase active sites was explored. An "all-in-one" pharmacophore model was created for the design of small molecules that may inhibit a broad spectrum of flaviviruses. This pharmacophore model approach serves as a robust cornerstone, thus assisting medicinal experts in the composition of multifunctional inhibitors that will eliminate cross-resistance and toxicity and enhance patient adherence.

Keywords: Binding landscape; Flaviviridae; Free-binding energy; NITD008; Pharmacophore model; RdRp.

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemistry
  • Adenosine / metabolism
  • Adenosine / pharmacology
  • Antiviral Agents / pharmacology*
  • Catalytic Domain
  • Drug Discovery / methods*
  • Flaviviridae / drug effects*
  • Flaviviridae / enzymology
  • Flaviviridae / physiology
  • Models, Chemical*
  • Molecular Docking Simulation
  • Molecular Dynamics Simulation
  • RNA-Dependent RNA Polymerase / drug effects*
  • RNA-Dependent RNA Polymerase / metabolism
  • Thermodynamics
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • NITD008
  • RNA-Dependent RNA Polymerase
  • Adenosine