Author: Ehmke, Veronika; Heindl, Cornelia; Rottmann, Matthias; Freymond, Céline; Schweizer, W. Bernd; Brun, Reto; Stich, August; Schirmeister, Tanja; Diederich, François
Title: Potent and Selective Inhibition of Cysteine Proteases from Plasmodium falciparum and Trypanosoma brucei Cord-id: g14kt2dv Document date: 2011_2_7
ID: g14kt2dv
Snippet: Treating tropical diseases: Structureâ€based design afforded highly active triazine nitrile inhibitors of the protozoan cysteine proteases falcipainâ€2 and rhodesain. Optimization of the occupancy of the S1, S2, and S3 pockets of these enzymes yielded inhibitory constants in the low nanomolar activity range. The new ligands are selective against other related proteases and exhibit in vitro activities against the protozoan parasites.[Image: see text]
Document: Treating tropical diseases: Structureâ€based design afforded highly active triazine nitrile inhibitors of the protozoan cysteine proteases falcipainâ€2 and rhodesain. Optimization of the occupancy of the S1, S2, and S3 pockets of these enzymes yielded inhibitory constants in the low nanomolar activity range. The new ligands are selective against other related proteases and exhibit in vitro activities against the protozoan parasites.[Image: see text]
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