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

Steverding, Dietmar, Wang, Xia ORCID: https://orcid.org/0000-0001-6915-2588, 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 β-lactone -γ- 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 3nM 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 -lactone - lactam proteasome inhibitors for rational anti-trypanosomal drug development.

Item Type:	Article
Uncontrolled Keywords:	β-lactone-γ-lactam proteasome inhibitors,sleeping sickness,trypanocidals,trypanosoma brucei,analytical chemistry,molecular medicine,pharmacology,pharmaceutical science,drug discovery,complementary and alternative medicine,organic chemistry,sdg 3 - good health and well-being ,/dk/atira/pure/subjectarea/asjc/1600/1602
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Related URLs:	http://www.scopus.com/inward/record.url?...
Depositing User:	Rhiannon Harvey
Date Deposited:	12 Dec 2011 15:48
Last Modified:	11 Nov 2024 17:30
URI:	https://ueaeprints.uea.ac.uk/id/eprint/35702
DOI:	10.1055/s-0031-1280315

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