β-arrestin-biased signaling by the β-adrenergic receptors.

摘要: Publisher Summary This chapter discusses β-arrestin-biased signaling by the β-adrenergic receptors. receptors (βARs) are considered prototypic members of superfamily cell-surface known as “seven-transmembrane receptors” (7TMRs aka G protein-coupled or GPCRs), which represented about a thousand genes in human genome. The physiological effects endogenous catecholamines, epinephrine (Epi) and norepinephrine (NE), mediated (βARs), large family 7TMRs. 7TMRs signal transducers for wide range extracellular stimuli that include hormones, neurotransmitters, lipids, peptides, ions, sensory stimuli. Their clinical importance is evident from fact 50% prescription drugs target this family. discovery β-arrestin-mediated has also revealed ligands can preferentially activate proteins versus β-arrestins vice versa, leading to behavior termed ‘‘biased agonism,’’ called ‘‘ligand-directed trafficking,’’ ‘‘protean ‘‘pleuridimensional efficacy,’’ ‘‘collateral efficacy’’.