title: β-arrestin-mediated signaling improves the efficacy of therapeutics.
abstract: β-Arrestins (β-arrestin-1 and β-arrestin-2) were first identified as proteins that have the ability to desensitize G protein-coupled receptors (GPCRs). However, it has recently been found that β-arrestins can activate signaling pathways independent of G protein activation. The diversity of these signaling pathways has also been recognized. This leads to an appreciation of β-arrestin-biased agonists, which is a new class of drugs that selectively activate β-arrestin-mediated signaling without G protein activation. In this review, we will discuss the recent advance of β-arrestin-mediated signaling pathways, including a brief account of different biased agonists, their pharmacological applications, and novel β-arrestin research.
authors.affiliation: Department of Pharmacology and Toxicology, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
authors.forename: Islam A A E-H
authors.initials: IA
authors.lastname: Ibrahim
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Kurose
mesh_terms: D000818:Animals; D019390:Arrestins / Q000819:agonists / Q000502:physiology*; D002227:Carbazoles / Q000494:pharmacology / Q000627:therapeutic use; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000503:physiopathology; D000077261:Carvedilol; D006801:Humans; D007211:Indoles / Q000494:pharmacology / Q000627:therapeutic use; D010879:Piperazines / Q000494:pharmacology / Q000627:therapeutic use; D011412:Propanolamines / Q000494:pharmacology / Q000627:therapeutic use; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000502:physiology; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology*; D016896:Treatment Outcome; D000071559:beta-Arrestin 1; D000071560:beta-Arrestin 2; D000071557:beta-Arrestins
chemical_list: C000605253:ARRB1 protein, human; C000605254:ARRB2 protein, human; D019390:Arrestins; D002227:Carbazoles; D007211:Indoles; D010879:Piperazines; D011412:Propanolamines; D043562:Receptors, G-Protein-Coupled; D000071559:beta-Arrestin 1; D000071560:beta-Arrestin 2; D000071557:beta-Arrestins; D000077261:Carvedilol; C484309:1-((5-chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine