GLP-2 analogue 10   Click here for help

GtoPdb Ligand ID: 9896

Immunopharmacology Ligand
Comment: This GLP-2 analogue (peptide 10 in [3]) was designed to increase the peptide's metabolic stability (and in vivo pharmacokinetic profile) beyond that of the clinically approved DPP4 resistant GLP-2 analogue teduglutide, with the aim of providing sustained therapeutic effects. GLP-2 analogue 10 achieves increased half-life by the incorporation of a covalent Cys-mediated side-chain cross-link (or staple) that stabilises the α-helical conformation of the peptide. The terminal PSSGAPPPS sequence of 10 is the C-terminal extension of exendin-4 which improves the peptide's solubility.
The intestinotrophic effects of GLP-2 (e.g. promotion of intestinal growth, reduced epithelial cell apoptosis and inflammation) has led to the development of GLP-2 analogues for the treatment of GI disorders such as short bowel syndrome, inflammatory bowel diseases and potentially other intestinal insufficiency diseases.
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1. Blonski W, Buchner AM, Aberra F, Lichtenstein G. (2013)
Teduglutide in Crohn's disease.
Expert Opin Biol Ther, 13 (8): 1207-14. [PMID:23834252]
2. Kochar B, Long MD, Shelton E, Young L, Farraye FA, Yajnik V, Herfarth H. (2017)
Safety and Efficacy of Teduglutide (Gattex) in Patients With Crohn's Disease and Need for Parenteral Support Due to Short Bowel Syndrome-associated Intestinal Failure.
J Clin Gastroenterol, 51 (6): 508-511. [PMID:27433811]
3. Yang PY, Zou H, Lee C, Muppidi A, Chao E, Fu Q, Luo X, Wang D, Schultz PG, Shen W. (2018)
Stapled, Long-Acting Glucagon-like Peptide 2 Analog with Efficacy in Dextran Sodium Sulfate Induced Mouse Colitis Models.
J Med Chem, 61 (7): 3218-3223. [PMID:29528634]