Title: β-Arrestin-Biased Signaling by the β-Adrenergic Receptors
Abstract: This chapter discusses β-arrestin-biased signaling by the β-adrenergic receptors. β-adrenergic receptors (βARs) are considered prototypic members of the superfamily of cell-surface receptors known as "seven-transmembrane receptors" (7TMRs aka G protein-coupled receptors or GPCRs), which are represented by about a thousand genes in the human genome. The physiological effects of endogenous catecholamines, epinephrine (Epi) and norepinephrine (NE), are mediated by the β-adrenergic receptors (βARs), which are members of the large family of 7TMRs. 7TMRs are signal transducers for a wide range of extracellular stimuli that include hormones, neurotransmitters, lipids, peptides, ions, and sensory stimuli. Their clinical importance is evident from the fact that about 50% of prescription drugs target members of this family. The discovery of β-arrestin-mediated signaling has also revealed that ligands can preferentially activate G proteins versus β-arrestins or vice versa, leading to a behavior termed as ''biased agonism,'' also called ''ligand-directed trafficking,'' ''protean agonism,'' ''pleuridimensional efficacy,'' and ''collateral efficacy''.
Publication Year: 2011
Publication Date: 2011-01-01
Language: en
Type: review
Indexed In: ['crossref', 'pubmed']
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Cited By Count: 11
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