The flavivirus protease as a target for drug discovery

Virol Sin. 2013 Dec;28(6):326-36. doi: 10.1007/s12250-013-3390-x. Epub 2013 Nov 14.

Abstract

Many flaviviruses are significant human pathogens causing considerable disease burdens, including encephalitis and hemorrhagic fever, in the regions in which they are endemic. A paucity of treatments for flaviviral infections has driven interest in drug development targeting proteins essential to flavivirus replication, such as the viral protease. During viral replication, the flavivirus genome is translated as a single polyprotein precursor, which must be cleaved into individual proteins by a complex of the viral protease, NS3, and its cofactor, NS2B. Because this cleavage is an obligate step of the viral life-cycle, the flavivirus protease is an attractive target for antiviral drug development. In this review, we will survey recent drug development studies targeting the NS3 active site, as well as studies targeting an NS2B/NS3 interaction site determined from flavivirus protease crystal structures.

Publication types

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

MeSH terms

  • Antiviral Agents / isolation & purification*
  • Antiviral Agents / pharmacology
  • Drug Discovery / methods*
  • Drug Discovery / trends
  • Flavivirus / drug effects*
  • Flavivirus / enzymology*
  • Humans
  • Protease Inhibitors / isolation & purification*
  • Protease Inhibitors / pharmacology
  • RNA Helicases / antagonists & inhibitors
  • Serine Endopeptidases
  • Viral Nonstructural Proteins / antagonists & inhibitors*

Substances

  • Antiviral Agents
  • NS2B protein, flavivirus
  • NS3 protein, flavivirus
  • Protease Inhibitors
  • Viral Nonstructural Proteins
  • Serine Endopeptidases
  • RNA Helicases