| Description |
-
Glucose-dependent insulinotropic peptide (GIP) is a 31-amino acid peptide hormone that is secreted by K-cells to regulate postprandial glucose levels. By binding to its receptor, GIPR, GIP mediates several beneficial effects such as improved insulin sensitivity, increased β-cell mass, and increased energy consumption. However, dipeptidyl peptidase-4 (DPP-4) rapidly inactivates GIP, within 5-7 min. ... read moreEfforts to extend DPP-4 targeted peptides have included inhibition of DPP-4 and lipidation of peptides. Here, synthesis of a N-trifluoroethyl and lipidated GIP was completed. The N-trifluoroethyl alkylation of GIP confers proteolytically resistant properties in vitro, providing complete resistance to overnight incubations with DPP-4. Compared to native GIP in vivo, the N-terminally protected and lipidated GIP remained in circulation at 800x and 80x higher concentrations, owing to the DPP-4 resistance and lipidiation.read less
|
|---|
This object is in collection
