Trypanocidal activity of β-lactone-γ-lactam proteasome inhibitors

Steverding, Dietmar, Wang, Xia, Potts, Barbara C. M. and Palladino, Michael A. (2012) Trypanocidal activity of β-lactone-γ-lactam proteasome inhibitors. Planta Medica, 78 (2). pp. 131-134. ISSN 0032-0943

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Abstract

Four beta-lactone-gamma-lactam proteasome inhibitors of natural origin were tested for their trypanocidal activities IN VITRO using culture-adapted bloodstream forms of TRYPANOSOMA BRUCEI. All four compounds displayed activities in the nanomolar range. The most trypanocidal compounds with 50?% growth inhibition (GI (50)) values of around 3 nM were the bromine and iodine analogues of salinosporamide A, a potent proteasome inhibitor produced by the marine actinomycete SALINISPORA TROPICA. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells. The data support the potential of beta-lactone-gamma-lactam proteasome inhibitors for rational anti-trypanosomal drug development.

Item Type:	Article
Faculty \ School:	Faculty of Medicine and Health Sciences > Norwich Medical School
UEA Research Groups:	Faculty of Medicine and Health Sciences > Research Groups > Gastroenterology and Gut Biology
Depositing User:	Rhiannon Harvey
Date Deposited:	12 Dec 2011 15:48
Last Modified:	11 Jan 2024 01:20
URI:	https://ueaeprints.uea.ac.uk/id/eprint/35702
DOI:	10.1055/s-0031-1280315

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