Trypanocidal activity of peptidyl vinyl ester derivatives selective for inhibition of mammalian proteasome trypsin-like activity

Steverding, Dietmar, Baldisserotto, Anna, Wang, Xia ORCID: https://orcid.org/0000-0001-6915-2588 and Marastoni, Mauro (2011) Trypanocidal activity of peptidyl vinyl ester derivatives selective for inhibition of mammalian proteasome trypsin-like activity. Experimental Parasitology, 128 (4). pp. 444-447. ISSN 1090-2449

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Abstract

Nine vinyl ester tripeptides selective for inhibition of mammalian proteasome trypsin-like activity were tested for in vitro activity against Trypanosoma brucei. Interestingly, two compounds showed trypanocidal activity in the low micromolar range without displaying cytotoxicity against human cells. However, the compounds did not inhibit the trypsin-like activity of the trypanosome proteasome although their effect correlates with inactivation of the chymotrypsin-like activity. This finding shows that the inhibitor sensitivities between mammalian and trypanosome proteasome are distinct. This difference may be exploited for rational anti-trypanosomal drug development.

Item Type:	Article
Additional Information:	Funding Information: We thank Dr Penny Powell for critical reading of the manuscript. This study was funded by a Seedcorn research grant from the Faculty of Health, University of East Anglia.
Uncontrolled Keywords:	proteasome,sleeping sickness,trypanosoma brucei,vinyl ester tripeptides,parasitology,immunology,infectious diseases,sdg 3 - good health and well-being ,/dk/atira/pure/subjectarea/asjc/2400/2405
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Related URLs:	http://www.scopus.com/inward/record.url?...
Depositing User:	Rhiannon Harvey
Date Deposited:	12 Dec 2011 15:22
Last Modified:	17 Nov 2024 07:30
URI:	https://ueaeprints.uea.ac.uk/id/eprint/35700
DOI:	10.1016/j.exppara.2011.03.015

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