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2018•Science SignalingRequires access

G protein–coupled receptor kinases (GRKs) orchestrate biased agonism at the β 2 -adrenergic receptor

Minjung Choi, Dean P. Staus, Laura M. Wingler, Seungkirl Ahn, Biswaranjan Pani, W. Darrell Capel, Robert J. Lefkowitz

Open publisher page 71 citations

Abstract

AR Y219A rescued both the initial recruitment of β-arrestin and its engagement with the intracellular core of the receptor. These data suggest that the Y219A mutation generates a G protein-biased state primarily by conformational selection against GRK coupling, rather than against β-arrestin. Together, these findings highlight the importance of GRKs in modulating the biased agonism of GPCRs.

About this research paper

What this paper is about

AR Y219A rescued both the initial recruitment of β-arrestin and its engagement with the intracellular core of the receptor. These data suggest that the Y219A mutation generates a G protein-biased state primarily by conformational selection against GRK coupling, rather than against β-arrestin. Together, these findings highlight the importance of GRKs in modulating the biased agonism of GPCRs.

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OpenAlex reports 71 citations for this work. Citation counts describe recorded attention and do not establish research quality.

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Available abstract

AR Y219A rescued both the initial recruitment of β-arrestin and its engagement with the intracellular core of the receptor. These data suggest that the Y219A mutation generates a G protein-biased state primarily by conformational selection against GRK coupling, rather than against β-arrestin. Together, these findings highlight the importance of GRKs in modulating the biased agonism of GPCRs.

Key concepts: G protein-coupled receptor kinase, Arrestin, G protein-coupled receptor, Beta adrenergic receptor kinase, Phosphorylation, Receptor, Cell biology, Kinase

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