Peptidomics applied: A new strategy for development of selective antagonists/agonists of insect pyrokinin (FXPRLamide) family using a novel conformational-mimetic motif

摘要

Applied peptidomics: A PK active core analog incorporating a novel transPro conformational-mimetic motif, the dihydroimidazole moiety, was found to demonstrate pure, selective agonism in pyrokinin (PK) family bioassays. A second PK core analog incorporating the dihydroimidazole moiety proved to be an antagonist of the diapause-termination activity of another PK assay. The dihydroimidazole analogs feature a modification adjacent to the primary tissue-bound peptidase hydrolysis site that is expected to enhance biostability over natural PK peptides identified by peptidomics. The research identifies a novel scaffold to design mimetic PK analogs as potential environmentally favorable pest management agents capable of disrupting PK-regulated systems.