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Design and evaluation of Trypanosoma brucei metacaspase inhibitors

Berg, M. and van der Veken, P. and Joossens, J. and Muthusamy, V. and Breugelmans, M. and Moss, C.X. and Rudolf, J. and Coombs, G.H. (2010) Design and evaluation of Trypanosoma brucei metacaspase inhibitors. Bioorganic and Medicinal Chemistry Letters, 20 (6). pp. 2001-2006. ISSN 0960-894X

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Abstract

Metacaspase (MCA) is an important enzyme in Trypanosoma brucei, absent from humans and differing significantly from the orthologous human caspases. Therefore MCA constitutes a new attractive drug target for antiparasitic chemotherapeutics, which needs further characterization to support the discovery of innovative drug candidates. A first series of inhibitors has been prepared on the basis of known substrate specificity and the predicted catalytic mechanism of the enzyme. In this Letter we present the first inhibitors of TbMCA2 with low micromolar enzymatic and antiparasitic activity in vitro combined with low cytotoxicity.

Item type: Article
ID code: 26122
Notes: Strathprints' policy is to record up to 8 authors per publication, plus any additional authors based at the University of Strathclyde. More authors may be listed on the official publication than appear in the Strathprints' record.
Keywords: trypanosoma brucei, metacaspase, inhibitor, african trypanosomiasis, sleeping sickness, protease inhibitor, Therapeutics. Pharmacology, Biochemistry, Organic Chemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Molecular Biology, Clinical Biochemistry
Subjects: Medicine > Therapeutics. Pharmacology
Department: Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
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Depositing user: Strathprints Administrator
Date Deposited: 20 Aug 2010 14:31
Last modified: 27 Mar 2014 09:03
URI: http://strathprints.strath.ac.uk/id/eprint/26122

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