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A cellular perspective of bias at G protein‐coupled receptors
Author(s) -
Fernandez Thomas J.,
De Maria Monica,
Lobingier Braden T.
Publication year - 2020
Publication title -
protein science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.353
H-Index - 175
eISSN - 1469-896X
pISSN - 0961-8368
DOI - 10.1002/pro.3872
Subject(s) - g protein coupled receptor , functional selectivity , receptor , agonist , signal transduction , microbiology and biotechnology , function (biology) , rhodopsin like receptors , cell function , biology , g protein , biophysics , chemistry , cell , biochemistry , metabotropic receptor
G protein‐coupled receptors (GPCRs) modulate cell function over short‐ and long‐term timescales. GPCR signaling depends on biochemical parameters that define the what, when, and where of receptor function: what proteins mediate and regulate receptor signaling, where within the cell these interactions occur, and how long these interactions persist. These parameters can vary significantly depending on the activating ligand. Collectivity, differential agonist activity at a GPCR is called bias or functional selectivity. Here we review agonist bias at GPCRs with a focus on ligands that show dramatically different cellular responses from their unbiased counterparts.

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