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Selectivity for G Protein or Arrestin-Mediated Signaling

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Functional Selectivity of G Protein-Coupled Receptor Ligands

Part of the book series: The Receptors ((REC))

Abstract

G protein-coupled receptors (GPCR) are expressed throughout the body in various cell types and organs. The cellular complement of proteins and the immediate scaffolds assembled in proximity to the receptor can determine how a receptor will signal in response to a given agonist. Furthermore, a particular agonist may promote receptor activation such that it favors interactions with different signaling partners within a cell. Therefore, a given receptor may have diverse functions depending on where it is expressed or what ligand is binding to it. β-arrestins are ubiquitously expressed cellular regulatory proteins that can play multifaceted roles in GPCR signaling. This chapter focuses on how different ligands can reveal differential roles of β-arrestins in determining GPCR signaling and regulation. We will focus on the neurotransmitter receptors for serotonin and opioids for specific examples of such functional selectivity.

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  1. Departments of Pharmacology and Psychiatry, The Ohio State University College of Medicine, Columbus, OH, 43210-1239

    Laura M. Bohn

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  1. Laura M. Bohn
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Correspondence to Laura M. Bohn .

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  1. VA Medical Center, 3710 SW US Veterans Hospital Road, 97239-2999, Portland, OR, USA

    Kim A. Neve

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Bohn, L.M. (2009). Selectivity for G Protein or Arrestin-Mediated Signaling. In: Neve, K.A. (eds) Functional Selectivity of G Protein-Coupled Receptor Ligands. The Receptors. Humana Press. https://doi.org/10.1007/978-1-60327-335-0_5

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