Author/Authors :
Roger Léger، نويسنده , , Karen Thibaudeau، نويسنده , , Martin Robitaille، نويسنده , , Omar Quraishi، نويسنده , , Pieter van Wyk، نويسنده , , Nathalie Bousquet-Gagnon، نويسنده , , Julie Carette، نويسنده , , Jean-Paul Castaigne، نويسنده , , Dominique P. Bridon، نويسنده ,
Abstract :
A series of analogs of GLP-1(7–36) amide containing a Nε-(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.
Keywords :
GLP-1 , DPP-IV.* Corresponding author. Tel.: +1-514-844-5558 , fax: +1-514-844-1119 , e-mail: leger@conjuchem.com , Albumin conjugate
