This proposal focus on finding new potential lead compounds to inhibit the trans-sialidase of Trypanosoma cruzi, as a step towards finding a drug against Chagas’ disease. A new high through-put enzyme assay will be used to scan a large library of small molecules and in combination with in silico pharmacophoric modelling this is expected to provide new types of scaffolds as well as identifying important functionalities in the ligand. Based on the obtained information a set of ligands will be designed. These ligands will be synthesised and further evaluated through the enzyme assay, kinetic and thermodynamical studies as well as structural studies. In an iterative optimization, these tools will be combined to obtain future generations of inhibitory ligands.
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