Antitrypanosomal activities of proteasome inhibitors

Antimicrob Agents Chemother. 2002 Jun;46(6):2038-40. doi: 10.1128/AAC.46.6.2038-2040.2002.

Abstract

Seven peptidyl proteasome inhibitors were tested for in vitro activity against Trypanosoma brucei bloodstream forms. Two compounds showed activity in the low nanomolar range. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells. The data support the potential of proteasome inhibitors for rational antitrypanosomal drug development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cysteine Endopeptidases
  • HL-60 Cells
  • Humans
  • Multienzyme Complexes / antagonists & inhibitors*
  • Proteasome Endopeptidase Complex
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects*
  • Trypanosomiasis / blood

Substances

  • Multienzyme Complexes
  • Trypanocidal Agents
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex