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Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Léger R,Thibaudeau K,Robitaille M,Quraishi O,van Wyk P,Bousquet-Gagnon N,Carette J,Castaigne JP,Bridon DP

doi

10.1016/j.bmcl.2004.06.066

subject

Has Abstract

pub_date

2004-09-06 00:00:00

pages

4395-8

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)00841-8

journal_volume

14

pub_type

杂志文章

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