Abstract
Aspartimide (Asi) formation is one of the most serious side reactions that can occur both during solid phase synthesis and storage of peptides containing aspartic acid. Although numerous studies on the mechanism of Asi formation conducted so far, the problem still remains unresolved and relatively little is known about the impact of this side reaction on biological properties of such modified peptides. In the present work we characterized the effect of Asi formation on biological properties of galanin(1-15) analogue modified in position 14 with aspartic acid, investigating its action on rat isolated gastric smooth muscles and glucose-induced insulin secretion from rat isolated islets of Langerhans. Our results show that this side process may adversely affect biological properties of such modified peptides. As we expected, modification of GAL(1-15)NH2 structure changed the interaction of GAL(1-15)NH2 with its receptors and consequently yielded peptide which, in studies on insulin secretion, showed insulinotropic- and antagonistic activities as compared to Asi-free analogue.
Keywords: Aspartimide, galanin analogue, insulin secretion, smooth muscle
Protein & Peptide Letters
Title: Aspartimide Modified Galanin Analogue Antagonizes Galanin Action on Insulin Secretion
Volume: 17 Issue: 10
Author(s): Jaroslaw Ruczynski, Zdzislaw Konstanski, Magdalena Cybal, Ivan Kocic and Piotr Rekowski
Affiliation:
Keywords: Aspartimide, galanin analogue, insulin secretion, smooth muscle
Abstract: Aspartimide (Asi) formation is one of the most serious side reactions that can occur both during solid phase synthesis and storage of peptides containing aspartic acid. Although numerous studies on the mechanism of Asi formation conducted so far, the problem still remains unresolved and relatively little is known about the impact of this side reaction on biological properties of such modified peptides. In the present work we characterized the effect of Asi formation on biological properties of galanin(1-15) analogue modified in position 14 with aspartic acid, investigating its action on rat isolated gastric smooth muscles and glucose-induced insulin secretion from rat isolated islets of Langerhans. Our results show that this side process may adversely affect biological properties of such modified peptides. As we expected, modification of GAL(1-15)NH2 structure changed the interaction of GAL(1-15)NH2 with its receptors and consequently yielded peptide which, in studies on insulin secretion, showed insulinotropic- and antagonistic activities as compared to Asi-free analogue.
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Ruczynski Jaroslaw, Konstanski Zdzislaw, Cybal Magdalena, Kocic Ivan and Rekowski Piotr, Aspartimide Modified Galanin Analogue Antagonizes Galanin Action on Insulin Secretion, Protein & Peptide Letters 2010; 17 (10) . https://dx.doi.org/10.2174/092986610792231447
DOI https://dx.doi.org/10.2174/092986610792231447 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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