Towards New Peptide-Based Therapeutics and Tools for Chemical Biology

Abstract

The majority of the thesis concerns the work conducted on nisin-derived semisynthetic lipopeptides. These compounds were evaluated for their antimicrobial activity and a selection of compounds showed to be as active as the parent compound nisin, while having superior stability, lower charge and lower molecular weight, making for an overall more drug-like entity. Further work was done on PRMT (Protein Arginine Methyl Transferase) peptide substrates comprising unnatural amino acids and their ability to tune PRMT activity. Finally, the synthesis of a fluorescent amino acid suitable for solid phase peptide synthesis is described, as well as a photocleavable linker, that can be of use in activity based protein profiling.