Synthesis of bifunctional peptide derivatives based on a β-cyclodextrin core with drug delivery potential
摘要:
A selective, versatile, robust methodology for bifunctionalization of beta-cyclodextrin is achieved allowing the attachment of peptides in varying C- and/or N-terminal combinations on resin using Fmoc SPPS. Two linkers are attached to cyclodextrin enabling selective binding to the resin (or a peptide attached to the resin). Continuation of peptide growth and/or cleavage from the resin follows, thus various combinations of peptide-cyclodextrin species are achieved. A model peptide (Gly-Ala) is used in this study to illustrate the potential of this system for attaching one or more bioactive peptides for drug transport and release purposes. (c) 2009 Elsevier Ltd. All rights reserved.