Hetero-bivalent GLP-1/glibenclamide for targeting pancreatic β-cells.

ABSTRACT: G protein-coupled receptor (GPCR) cell signalling cascades are initiated upon binding of a specific agonist ligand to its cell surface receptor. Linking multiple heterologous ligands that simultaneously bind and potentially link different receptors on the cell surface is a unique approach to modulate cell responses. Moreover, if the target receptors are selected based on analysis of cell-specific expression of a receptor combination, then the linked binding elements might provide enhanced specificity of targeting the cell type of interest, that is, only to cells that express the complementary receptors. Two receptors whose expression is relatively specific (in combination) to insulin-secreting pancreatic β-cells are the sulfonylurea-1 (SUR1) and the glucagon-like peptide-1 (GLP-1) receptor

SUBMITTER: Hart NJ 

PROVIDER: S-EPMC4100979 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature