exendin-phe1

exendin-phe1 (ExF1) is a peptide-based biased agonist of the glucagon-like peptide-1 receptor (GLP-1R), primarily used as a pharmacological tool to study the spatial dynamics of G protein-coupled receptor (GPCR) signaling. It is a modified analog of exendin-4, where the N-terminal histidine is replaced with phenylalanine. This substitution results in a ligand that maintains the ability to stimulate cAMP production but exhibits significantly slower receptor internalization compared to native GLP-1 or other analogs like exendin-asp3. By remaining localized at the cell surface, exendin-phe1 allows researchers to differentiate between plasma membrane-initiated signaling and endosomal signaling. Its development is centered on understanding how biased agonism can be optimized to improve insulin secretion and therapeutic outcomes in metabolic disorders such as type 2 diabetes and obesity.

Other names

[Phe1]exendin-4Phe1-exendin-4Phe-1-exendin-4Phe 1-exendin-4