Teaching old receptors new tricks: biasing seven-transmembrane receptors.

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Published in Nat Rev Drug Discov on May 01, 2010

Authors

Sudarshan Rajagopal1, Keshava Rajagopal, Robert J Lefkowitz

Author Affiliations

1: Department of Medicine, Duke University Medical Center, 2301 Erwin Road, Durham, North Carolina 27710, USA.

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Quantifying ligand bias at seven-transmembrane receptors. Mol Pharmacol (2011) 2.08

Distinct conformational changes in beta-arrestin report biased agonism at seven-transmembrane receptors. Proc Natl Acad Sci U S A (2008) 2.06

Dopaminergic supersensitivity in G protein-coupled receptor kinase 6-deficient mice. Neuron (2003) 2.03

Beta-arrestin2-mediated inotropic effects of the angiotensin II type 1A receptor in isolated cardiac myocytes. Proc Natl Acad Sci U S A (2006) 2.01

Differential mechanisms of morphine antinociceptive tolerance revealed in (beta)arrestin-2 knock-out mice. J Neurosci (2002) 2.01

beta-Arrestin inhibits NF-kappaB activity by means of its interaction with the NF-kappaB inhibitor IkappaBalpha. Proc Natl Acad Sci U S A (2004) 1.91

Trafficking patterns of beta-arrestin and G protein-coupled receptors determined by the kinetics of beta-arrestin deubiquitination. J Biol Chem (2003) 1.90

Reciprocal regulation of angiotensin receptor-activated extracellular signal-regulated kinases by beta-arrestins 1 and 2. J Biol Chem (2004) 1.86

Beta-arrestin-2 regulates the development of allergic asthma. J Clin Invest (2003) 1.85

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands. Proc Natl Acad Sci U S A (2009) 1.84

Arrestin development: emerging roles for beta-arrestins in developmental signaling pathways. Dev Cell (2009) 1.83

beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice. J Clin Invest (2009) 1.79

Beta-arrestin1 mediates insulin-like growth factor 1 (IGF-1) activation of phosphatidylinositol 3-kinase (PI3K) and anti-apoptosis. J Biol Chem (2003) 1.76

Activation-dependent conformational changes in {beta}-arrestin 2. J Biol Chem (2004) 1.76

Regulation of G protein-coupled receptor signaling by scaffold proteins. Circ Res (2002) 1.75

beta-Arrestin 1 and Galphaq/11 coordinately activate RhoA and stress fiber formation following receptor stimulation. J Biol Chem (2004) 1.75

G-protein-coupled receptor kinase specificity for beta-arrestin recruitment to the beta2-adrenergic receptor revealed by fluorescence resonance energy transfer. J Biol Chem (2006) 1.73

beta -Arrestins regulate protease-activated receptor-1 desensitization but not internalization or Down-regulation. J Biol Chem (2001) 1.70

Protein kinase A and G protein-coupled receptor kinase phosphorylation mediates beta-1 adrenergic receptor endocytosis through different pathways. J Biol Chem (2003) 1.66

Oxygen-regulated beta(2)-adrenergic receptor hydroxylation by EGLN3 and ubiquitylation by pVHL. Sci Signal (2009) 1.66

A stress response pathway regulates DNA damage through β2-adrenoreceptors and β-arrestin-1. Nature (2011) 1.64

Global phosphorylation analysis of beta-arrestin-mediated signaling downstream of a seven transmembrane receptor (7TMR). Proc Natl Acad Sci U S A (2010) 1.64

S-nitrosylation of beta-arrestin regulates beta-adrenergic receptor trafficking. Mol Cell (2008) 1.63

{beta}-Arrestin-2 Mediates Anti-apoptotic Signaling through Regulation of BAD Phosphorylation. J Biol Chem (2009) 1.59

Independent beta-arrestin2 and Gq/protein kinase Czeta pathways for ERK stimulated by angiotensin type 1A receptors in vascular smooth muscle cells converge on transactivation of the epidermal growth factor receptor. J Biol Chem (2009) 1.57

Arresting developments in heptahelical receptor signaling and regulation. Trends Cell Biol (2002) 1.55

Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation. Nature (2016) 1.55

Spinophilin blocks arrestin actions in vitro and in vivo at G protein-coupled receptors. Science (2004) 1.52

Regulation of V2 vasopressin receptor degradation by agonist-promoted ubiquitination. J Biol Chem (2003) 1.50

Protein kinase A-mediated phosphorylation of the beta 2-adrenergic receptor regulates its coupling to Gs and Gi. Demonstration in a reconstituted system. J Biol Chem (2002) 1.50

Enhanced rewarding properties of morphine, but not cocaine, in beta(arrestin)-2 knock-out mice. J Neurosci (2003) 1.49

Beta-arrestin-dependent signaling and trafficking of 7-transmembrane receptors is reciprocally regulated by the deubiquitinase USP33 and the E3 ligase Mdm2. Proc Natl Acad Sci U S A (2009) 1.49

Receptor-specific ubiquitination of beta-arrestin directs assembly and targeting of seven-transmembrane receptor signalosomes. J Biol Chem (2005) 1.47

Prolonged kappa opioid receptor phosphorylation mediated by G-protein receptor kinase underlies sustained analgesic tolerance. J Biol Chem (2003) 1.45

The use of lung donors older than 55 years: a review of the United Network of Organ Sharing database. J Heart Lung Transplant (2013) 1.42

Constitutive protease-activated receptor-2-mediated migration of MDA MB-231 breast cancer cells requires both beta-arrestin-1 and -2. J Biol Chem (2004) 1.41

The active conformation of beta-arrestin1: direct evidence for the phosphate sensor in the N-domain and conformational differences in the active states of beta-arrestins1 and -2. J Biol Chem (2007) 1.41

beta-Arrestin-dependent constitutive internalization of the human chemokine decoy receptor D6. J Biol Chem (2004) 1.39

Smoothened signal transduction is promoted by G protein-coupled receptor kinase 2. Mol Cell Biol (2006) 1.38

Beta-arrestins regulate atherosclerosis and neointimal hyperplasia by controlling smooth muscle cell proliferation and migration. Circ Res (2008) 1.37

Marginal cardiac allografts do not have increased primary graft dysfunction in alternate list transplantation. Circulation (2006) 1.37

Beta-arrestin and Mdm2 mediate IGF-1 receptor-stimulated ERK activation and cell cycle progression. J Biol Chem (2007) 1.36

Ubiquitination of beta-arrestin links seven-transmembrane receptor endocytosis and ERK activation. J Biol Chem (2007) 1.34

Beta-arrestin 2-dependent angiotensin II type 1A receptor-mediated pathway of chemotaxis. Mol Pharmacol (2005) 1.33

{beta}-Arrestin is crucial for ubiquitination and down-regulation of the insulin-like growth factor-1 receptor by acting as adaptor for the MDM2 E3 ligase. J Biol Chem (2005) 1.31

Neuropathic pain activates the endogenous kappa opioid system in mouse spinal cord and induces opioid receptor tolerance. J Neurosci (2004) 1.26

Phosphorylation of beta-arrestin2 regulates its function in internalization of beta(2)-adrenergic receptors. Biochemistry (2002) 1.24

When 7 transmembrane receptors are not G protein-coupled receptors. J Clin Invest (2005) 1.24

Src-dependent tyrosine phosphorylation regulates dynamin self-assembly and ligand-induced endocytosis of the epidermal growth factor receptor. J Biol Chem (2002) 1.24

G-protein receptor kinase 3 (GRK3) influences opioid analgesic tolerance but not opioid withdrawal. Br J Pharmacol (2003) 1.23