Publication
Title
Design and evaluation of **Trypanosoma brucei** metacaspase inhibitors
Author
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.
Language
English
Source (journal)
Bioorganic and medicinal chemistry letters. - Oxford
Publication
Oxford : 2010
ISSN
0960-894X
Volume/pages
20:6(2010), p. 2001-2006
ISI
000275221500045
Full text (Publisher's DOI)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 08.03.2010
Last edited 11.10.2017
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