Optimization of small-molecule probes or drugs is a synthetically lengthy, challenging, and resource-intensive process. Lack of automation and reliance on skilled medicinal chemists is cumbersome in both academic and industrial settings. Here, we demonstr
Cappiello, John R.,Chen, Emily,Dillon, Nicholas,Hull, Mitchell V.,Kitamura, Seiya,Kitamura, Shinichi,Kotaniguchi, Miyako,Nizet, Victor,Sharpless, K. Barry,Solania, Angelo,Woehl, Jordan L.,Wolan, Dennis W.,Zheng, Qinheng
Design and evaluation of Trypanosoma brucei metacaspase inhibitors
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.
Berg, Maya,Veken, Pieter Van der,Joossens, Jurgen,Muthusamy, Venkatraj,Breugelmans, Matthias,Moss, Catherine X.,Rudolf, Jana,Cos, Paul,Coombs, Graham H.,Maes, Louis,Haemers, Achiel,Mottram, Jeremy C.,Augustyns, Koen
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(2010/10/01)
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