Novel lipoamino acid- and liposaccharide-based system for peptide delivery: Application for oral administration of tumor-selective somatostatin analogues

István Tóth, John P. Malkinson, Nicholas S. Flinn, Bruno Drouillat, Anikó Horváth, Judith Érchegyi, Miklós Idei, Anikó Venetianer, Per Artursson, Lucia Lazorova, Béla Szende, György Kéri

Research output: Contribution to journalArticle

42 Citations (Scopus)

Abstract

Lipoamino acid and liposaccharide conjugates of somatostatin analogue TT-232 were synthesized to modify the physicochemical properties of the parent peptide. The relative position, the number, and the nature of the lipid and/or saccharide moieties were varied. Experiments in vitro clearly showed that many compounds modified at the N- and/or C-terminus with lipid or sugar moieties retained the biological activity of the parent compound. An interesting construct was synthesized containing lipid and sugar units at opposite ends of the somatostatin analogue, so that the entire molecule could be considered as an amphipathic surfactant.

Original languageEnglish
Pages (from-to)4010-4013
Number of pages4
JournalJournal of Medicinal Chemistry
Volume42
Issue number19
DOIs
Publication statusPublished - Sep 23 1999

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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