Chemical Proteomics for Target Discovery of Head-to-Tail Cyclized Mini-Proteins.

ABSTRACT: Target deconvolution is one of the most challenging tasks in drug discovery, but a key step in drug development. In contrast to small molecules, there is a lack of validated and robust methodologies for target elucidation of peptides. In particular, it is difficult to apply these methods to cyclic and cysteine-stabilized peptides since they exhibit reduced amenability to chemical modification and affinity capture; however, such ribosomally synthesized and post-translationally modified peptide natural products are rich sources of promising drug candidates. For example, plant-derived circular peptides called cyclotides have recently attracted much attention due to their immunosuppressive effects and oral activity in the treatment of multiple sclerosis in mice, but their molecular target has

SUBMITTER: Hellinger R 

PROVIDER: S-EPMC5641551 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature