Abstract
Bi-nuclear amino acid platforms loaded with various drugs for conjugation to a peptide carrier were synthesized using simple and convenient orthogonally protective solid-phase organic synthesis (SPOS). Each arm of the platform carries a different anticancer agent linked through the same or different functional group, providing discrete chemo- and bio-release profiles for each drug, and also enabling "switch off/switch on" regulation of drug cytotoxicity by conjugation to the platform and to a cell targeting peptide. The versatility of this approach enables efficient production of drug-loaded platforms and determination of favorable drug combinations/modes of linkage for subsequent conjugation to a carrier moiety for targeted cancer cell therapy. The results presented here potentiate the application of amino acid platforms for targeted drug delivery (TDD).
Original language | English |
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Pages (from-to) | 139-146 |
Number of pages | 8 |
Journal | European Journal of Medicinal Chemistry |
Volume | 85 |
DOIs | |
State | Published - 6 Oct 2014 |
Keywords
- Amino acid platform
- Controlled drug release
- Peptide-drug conjugates
- Prodrug
- Solid phase organic synthesis