Abstract：
:The natural compound tyropeptin A, a new peptidyl aldehyde proteasome inhibitor, was tested for its trypanocidal activity in vitro using culture-adapted bloodstream forms of Trypanosoma brucei. The concentrations of tyropeptin A required to reduce the growth rate by 50 % and to kill all cells were 10 and 100 times lower for bloodstream-form trypanosomes than for human leukaemia HL-60 cells, respectively. Enzymatic analysis showed that the trypsin-like activity of the trypanosome proteasome and the chymotrypsin-like activity of the mammalian proteasome are particularly sensitive to inhibition by tyropeptin A. The results suggest that natural compounds targeting the trypsin-like activity of the proteasome may serve as leads for rational drug development of novel anti-trypanosomal agents.
journal_name
Planta Medjournal_title
Planta medicaauthors
Steverding D,Pemberton AJ,Royle H,Spackman RW,Rivett AJdoi
10.1055/s-2006-931600subject
Has Abstractpub_date
2006-06-01 00:00:00pages
761-3issue
8eissn
0032-0943issn
1439-0221journal_volume
72pub_type
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