GLP-2 analogue 10   Click here for help

GtoPdb Ligand ID: 9896

Immunopharmacology Ligand
Compound class: Peptide or derivative
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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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
GLP-2 analogue 10 exhibits more effective anti-inflammatory effects in mouse models of DSS-induced colitis than teduglutide [3]. The half-life of GLP-2 analogue 10 is 4.7 hours after i.v. administration, in contrast to teduglutide's half-life of 25 minutes.
Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
GLP-2 receptor Hs Agonist Agonist 10.6 pEC50 - 3
⤷ pEC50 10.6 (EC50 2.8x10-11 M) [3]
Description: Determined in a reporter assay using HEK293 cells stably overexpressing a cAMP response element (CRE) driven luciferase reporter and human GLP-2R.