Development of Generic G Protein Peptidomimetics Able to Stabilize Active State G(s) Protein-Coupled Receptors for Application in Drug Discovery Vrije Universiteit Brussel
G protein-coupled receptors (GPCRs) represent an important group of membrane proteins that play a central role in modern medicine. Unfortunately, conformational promiscuity hampers full therapeutic exploitation of GPCRs, since the largest population of the receptor will adopt a basal conformation, which subsequently challenges screens for agonist drug discovery programs. Herein, we describe a set of peptidomimetics able to mimic the ability ...