The synthesis of three first-order dendrimers based on a b-cyclodextrin core containing fourteen Val, Phe and Val-Phe residues is described. The guest binding ability of the tetradecavalent peptidyl b-cyclodextrin derivative has been tested by calorimetric titration and the thermodynamic parameters
Synthesis of bifunctional peptide derivatives based on a β-cyclodextrin core with drug delivery potential
✍ Scribed by Rachel J. White; Paul G. Plieger; David R.K. Harding
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- French
- Weight
- 397 KB
- Volume
- 51
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
A selective, versatile, robust methodology for bifunctionalization of b-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.
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