Novel Lipoamino Acid- and Liposaccharide-Based System for Peptide Delivery:  Application for Oral Administration of Tumor-Selective Somatostatin Analogues

Toth, I., Malkinson, J.P., Flinn, N.S., Drouillat, B., Horvath, A., Erchegyi, J., Idei, M., Venetianer, A., Artursson, P., Lazorova, L., Szende, B. and Keri, G. (1999) Novel Lipoamino Acid- and Liposaccharide-Based System for Peptide Delivery:  Application for Oral Administration of Tumor-Selective Somatostatin Analogues. Journal of Medicinal Chemistry, 42 (19). pp. 4010-4013. 10.1021/jm9910167.

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DOI: 10.1021/jm9910167

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.

Item Type:Article
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2404
Journal or Publication Title:Journal of Medicinal Chemistry
Deposited By:Library Staff
Deposited On:03 Nov 2011 17:39
Last Modified:03 Nov 2011 17:39

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