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
Depositing User: Rhiannon Harvey
Date Deposited: 12 Dec 2011 15:48
Last Modified: 04 Aug 2020 23:26
URI: https://ueaeprints.uea.ac.uk/id/eprint/35702
DOI: 10.1055/s-0031-1280315

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