Glycosylation of Pramlintide: Synthetic Glycopeptides that Display In Vitro and In Vivo Activities as Amylin Receptor Agonists

Abstract

Sweet medicine: Glycosylated analogues of pramlintide, in which specific Asn residues bear extended N-glycan structures, may be accessed by a combination of solid-phase peptide synthesis and highly efficient enzymatic glycosylation (see scheme; ENGases=endo-β-N-acetylglucosaminidases). Glycopeptides display both in vitro and in vivo activity as amylin receptor agonists and effect ‘smoothing’ of blood glucose.