title: Antitrypanosomal activities of proteasome inhibitors.
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.
authors.affiliation: Abteilung Parasitologie, Hygiene-Institut. Institut für Pharmazeutische Biologie, Ruprecht-Karls-Universität, Heidelberg, Germany.
authors.forename: Njinkeng Joseph
authors.initials: NJ
authors.lastname: Nkemngu
authors.forename: Joseph
authors.initials: J
authors.lastname: Nkemgu-Njinkeng
authors.forename: Vera
authors.initials: V
authors.lastname: Rosenkranz
authors.forename: Michael
authors.initials: M
authors.lastname: Wink
authors.forename: Dietmar
authors.initials: D
authors.lastname: Steverding
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D003546:Cysteine Endopeptidases; D018922:HL-60 Cells; D006801:Humans; D009097:Multienzyme Complexes / Q000037:antagonists & inhibitors*; D046988:Proteasome Endopeptidase Complex; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*; D014352:Trypanosomiasis / Q000097:blood
chemical_list: D009097:Multienzyme Complexes; D014344:Trypanocidal Agents; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex