Berg, M. et al. (2010) Design and evaluation of Trypanosoma brucei metacaspase inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(6), pp. 2001-2006. (doi: 10.1016/j.bmcl.2010.01.099)
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Publisher's URL: http://dx.doi.org/10.1016/j.bmcl.2010.01.099
Abstract
Metacaspase (MCA) is an important enzyme in <i>Trypanosoma brucei</i>, 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: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Moss, Dr Catherine and Mottram, Professor Jeremy and Coombs, Professor Graham and Rudolf, Dr Jana |
| Authors: | Berg, M., Van der Veken, P., Joossens, J., Muthusamy, V., Breugelmans, M., Moss, C. X., Rudolf, J., Cos, P., Coombs, G. H., Maes, L., Haemers, A., Mottram, J. C., and Augustyns, K. |
| Subjects: | Q Science > QH Natural history > QH345 Biochemistry |
| College/School: | College of Medical Veterinary and Life Sciences > School of Infection & Immunity |
| Journal Name: | Bioorganic and Medicinal Chemistry Letters |
| ISSN: | 0960-894X |
| ISSN (Online): | 1464-3405 |
| Published Online: | 25 January 2010 |
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