Chemical Ligands and Methods A2: Natural products as starting structures for the development of supramolecular ligands

Prof. Dr. Markus Kaiser

Project A2 starts from naturally occuring cyclodepsipeptides and turns them into highly specific inhibitors of S1-serine proteases. Suitable derivatizations are obtained from biochemical digestion experiments or via virtual docking to the specificity pockets known from crystal structures, and are subsequently realized by total synthesis. In order to produce powerful ditopic receptor molecules for neighbouring protein domains, dynamic combinatorial chemistry will merge two series of specific binders and select those building blocks with a perfect match on both binding epitopes.