Complexity in influenza virus targeted drug design: interaction with human sialidases

J Med Chem. 2010 Apr 8;53(7):2998-3002. doi: 10.1021/jm100078r.

Abstract

With the global spread of the pandemic H1N1 and the ongoing pandemic potential of the H5N1 subtype, the influenza virus represents one of the most alarming viruses spreading worldwide. The influenza virus sialidase is an effective drug target, and a number of inhibitors are clinically effective against the virus (zanamivir, oseltamivir, peramivir). Here we report structural and biochemical studies of the human cytosolic sialidase Neu2 with influenza virus sialidase-targeting drugs and related compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Crystallography, X-Ray
  • Drug Design*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / metabolism*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Influenza A Virus, H1N1 Subtype / enzymology
  • Influenza A Virus, H5N1 Subtype / enzymology
  • Models, Molecular
  • Molecular Conformation
  • Neuraminidase / antagonists & inhibitors*
  • Neuraminidase / chemistry
  • Neuraminidase / metabolism
  • Orthomyxoviridae / enzymology*

Substances

  • Enzyme Inhibitors
  • NEU2 protein, human
  • Neuraminidase

Associated data

  • PDB/2F0Z
  • PDB/2F10
  • PDB/2F11
  • PDB/2F12
  • PDB/2F13