| Literature DB >> 15183905 |
Cyril Sarrauste de Menthière1, Alain Chavanieu, Gérard Grassy, Stéphane Dalle, Guillermo Salazar, Alain Kervran, Bruno Pfeiffer, Pierre Renard, Philippe Delagrange, Dominique Manechez, David Bakes, Alain Ktorza, Bernard Calas.
Abstract
A series of GLP-1-[7-36]-NH(2) (tGLP-1) and GLP-1-[7-37] analogs modified in position 7, 8, 9 and 36, have been designed and evaluated on murine GLP-1 receptors expressed in RIN T3 cells for both their affinity and activity. Ten of the synthesized peptides were found full agonists with activities superior or at least equal to that of the native hormone. Five of them were investigated for their plasmatic stability and the most stable, [a(8)-desR(36)]GLP-1-[7-37]- NH(2) (Compound 8), evaluated in vivo in a glucose tolerance test which confirmed a clearly longer activity than that of the native hormone. We also performed circular dichroism study and propose a hypothetical structural model explaining the most part of observed activities of GLP-1 analogs on RIN T3 cells.Entities:
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Year: 2004 PMID： 15183905 DOI： 10.1016/j.ejmech.2004.02.002
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514