Agonist-selective signaling or ligand-biased signaling of G protein-coupled receptor (GPCR) has become the focus of an increasing number of laboratories. The principle of this concept is that agonist possesses different abilities to activate different signaling pathways. Current review summarizes the observations of agonist-selective signaling of various GPCRs, indicating the significance of agonist-selective signaling in biological processes. In addition, current review also provides an overview on how agonist-selective signaling is initiated. Especially, the relationship between GPCR-G protein interaction and GPCR-beta-arrestin interaction is discussed in depth.
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