2. Academic Validation
  3. Structural requirements of the N-terminal region of GLP-1-[7-37]-NH2 for receptor interaction and cAMP production

Structural requirements of the N-terminal region of GLP-1-[7-37]-NH2 for receptor interaction and cAMP production

  • Eur J Med Chem. 2004 Jun;39(6):473-80. doi: 10.1016/j.ejmech.2004.02.002.
Cyril Sarrauste de Menthière 1,  Alain Chavanieu,  Gérard Grassy,  Stéphane Dalle,  Guillermo Salazar,  Alain Kervran,  Bruno Pfeiffer,  Pierre Renard,  Philippe Delagrange,  Dominique Manechez,  David Bakes,  Alain Ktorza,  Bernard Calas
Affiliations

Affiliation

  • 1 Centre de Biochimie Structurale, CNRS UMR 5048 - UM1 - INSERM UMR 554, 29 rue de Navacelles, 34090 Montpellier Cedex, France.
PMID: 15183905 DOI: 10.1016/j.ejmech.2004.02.002
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.

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