Peptidic dual GLP-1 / glucagon receptor agonists derived from exendin-4
Patent Information
- Authority / Receiving Office
- CN · China
- Current Assignee / Owner
- SANOFI SA
- Publication Date
- 2017-02-15
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Abstract
Description
[0001] field of invention
[0002] The present invention relates to exendin-4 (exendin-4) peptide analogs, which activate glucagon-like peptide-1 (GLP-1) and glucagon (GCG) receptors and optionally glucose- Dependent insulinotropic polypeptide (GIP) receptors, and their medical uses, for example in the treatment of disorders of the metabolic syndrome (including diabetes and obesity) and in reducing excess food intake.
[0003] Background of the invention
[0004] Exendin-4 is a 39-amino acid peptide produced by the salivary glands of the monster monster (Heloderma suspectum) (Eng J. et al., J. Biol. Chem., 1992, 267, 7402- 05). Exendin-4 is an activator of the glucagon-like peptide-1 (GLP-1) receptor, but it shows only very low activation of the GIP receptor and does not activate the glucagon receptor (see Table 1).
[0005] Table 1: Potency (expressed in pM) of increasing concentrations of exendin-4 on GLP-1, GIP and glucagon receptors and cAMP formed measured as described ...