Antitrypanosomal activities of proteasome inhibitors.
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.
Nkemngu
Njinkeng Joseph
NJ
Abteilung Parasitologie, Hygiene-Institut. Institut für Pharmazeutische Biologie, Ruprecht-Karls-Universität, Heidelberg, Germany.
Nkemgu-Njinkeng
Joseph
J
Rosenkranz
Vera
V
Wink
Michael
M
Steverding
Dietmar
D
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
D009097:Multienzyme Complexes; D014344:Trypanocidal Agents; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex