Exploring Diverse Signaling Mechanisms of G Protein-Coupled Receptors through Structural Biology

Abstract Recent advancements in structural biology have facilitated the elucidation of complexes involving G protein-coupled receptors (GPCRs) and their associated signal transducers, including G proteins and arrestins. A comprehensive analysis of these structures provides profound insights into the dynamics of signaling mechanisms. These structural revelations can potentially guide the development of drugs to minimize side effects through targeted and selective signaling. Understanding the binding modes of different signal-selective ligands is imperative for future drug research and development. Here, we conduct a comparative examination of the structural details of various GPCR–signal transducer complexes and delve into the molecular basis of the currently proposed signal selectivity.