β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors

By M. Azzi, Pascale G. Charest, S. Angers, G. Rousseau, T. Kohout, Michel Bouvier, G. Piñeyro. Proceedings of the National Academy of Sciences of the United States of America, 2003

479 citations recorded by the source corpus.

Subfields: Cellular and Molecular Neuroscience, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/53e1193a1996eeac1a6de601f817265299250db0

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Citations in the corpus

G protein coupled receptor structure and activation. (2007, background): “Moreover, there is a growing appreciation that GPCR regulation and signaling is much more complex than originally envisioned, and includes signalling through G protein independent pathways [2–4].”
Lifting the lid on GPCRs: the role of extracellular loops (2011, background): “Individual GPCRs can activate multiple types of G-protein, not just one type, and signalling can be G-protein independent, such as b-arrestin-dependent GPCR activation of MAPK (Azzi et al., 2003).”
A G Protein-Biased Ligand at the μ-Opioid Receptor Is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with Morphine (2013, background): “…including coupling to different Ga subunits (Spengler et al., 1993; Eason et al., 1994), and between G protein coupling and b-arrestin recruitment (Azzi et al., 2003; Gesty-Palmer et al., 2006; DeWire et al., 2007; Violin and Lefkowitz, 2007; Kim et al., 2008; Ma et al., 2009; Gesty-Palmer and…”
Regulation of µ-Opioid Receptors: Desensitization, Phosphorylation, Internalization, and Tolerance (2013, background): “b2-adrenergic receptor, an inverse agonist not only suppressed the constitutive activity of the receptors but also activated MAPK via a b-arrestin2-dependent mechanism (Azzi et al., 2003).”
Conformational complexity of G-protein-coupled receptors. (2007, background): “Structurally different agonists disrupt distinct combinations of stabilizing intramolecular interactions Evidence from both cell-based and biophysical studies suggests that structurally different agonists (and partial agonists) of a given GPCR can induce distinct conformational states, rather than s”