| Literature DB >> 15357960 |
Roger Léger1, Karen Thibaudeau, Martin Robitaille, Omar Quraishi, Pieter van Wyk, Nathalie Bousquet-Gagnon, Julie Carette, Jean-Paul Castaigne, Dominique P Bridon.
Abstract
A series of analogs of GLP-1(7-36) amide containing a Nepsilon-(2-[2-[2-(3-maleimidopropylamido)ethoxy]ethoxy]acetyl)lysine has been synthesized and the resulting derivatives were bioconjugated to Cys34 of human serum albumin (HSA). The GLP-1-HSA bioconjugates were analyzed in vitro to assess the stabilizing effect of bioconjugation in the presence of DPP-IV as well as GLP-1 receptor binding and activation. Compound 9 (CJC-1131) having the point of attachment to albumin at the C-terminal of GLP-1 and a D-alanine substitution at position 8 was identified as having the best combination of stability and bioactivity.Entities:
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Year: 2004 PMID： 15357960 DOI： 10.1016/j.bmcl.2004.06.066
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823