ABSTRACT
The demand for peptide drugs is increasing and in this context, "post-assembly (or post-translational) peptide modification strategies" by chemical manipulation of intact oligo-peptides has provided several analogues. Compounds prepared by this method are useful therapeutic molecules for structure activity studies. Herein, we describe various chemical methods such as cross-coupling reactions, cycloaddition reactions, radical reactions and ring-closing metathesis reactions that are useful for post-translational peptide modifications.
Subject(s)
Oligopeptides/chemistry , Oligopeptides/chemical synthesis , Pharmaceutical Preparations/chemistry , Pharmaceutical Preparations/chemical synthesis , Molecular StructureABSTRACT
We have demonstrated an exceptionally simple and a useful methodology for modification of unusual phenylalanine peptides by adapting the building block approach using the Suzuki-Miyaura cross-coupling reaction as a key step. This strategy gave a good overall yield of various modified tri- and pentapeptides that may be useful to prepare various biologically active peptides in a short period of time.
