"Switch off/switch on" regulation of drug cytotoxicity by conjugation to a cell targeting peptide

Yossi Gilad, Michael A. Firer, Alex Rozovsky, Elena Ragozin, Boris Redko, Amnon Albeck, Gary Gellerman

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

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 languageEnglish
Pages (from-to)139-146
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume85
DOIs
StatePublished - 6 Oct 2014

Keywords

  • Amino acid platform
  • Controlled drug release
  • Peptide-drug conjugates
  • Prodrug
  • Solid phase organic synthesis

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