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You searched for: Subject "G-protein coupled receptors" Remove constraint Subject: "G-protein coupled receptors" Journal Cell Remove constraint Journal: Cell Publication Year 2016 Remove constraint Publication Year: 2016 Subject G-protein coupled receptors Remove constraint Subject: G-protein coupled receptors Subject agonists Remove constraint Subject: agonists
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1. Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy

Author:
Furness, Sebastian George Barton; Liang, Yi-Lynn; Nowell, Cameron James; Halls, Michelle Louise; Wookey, Peter John; Dal Maso, Emma; Inoue, Asuka; Christopoulos, Arthur; Wootten, Denise; Sexton, Patrick Michael
Source:
Cell 2016 v.167 pp. 739-749.e11
ISSN:
0092-8674
Subject:
G-protein coupled receptors,   etc   ; agonists; calcitonin; drugs; guanosine triphosphate; ligands; protein conformation; second messengers;     Show all 8 Subjects
Abstract:
... G protein-coupled receptor (GPCR) signaling, mediated by hetero-trimeric G proteins, can be differentially controlled by agonists. At a molecular level, this is thought to occur principally via stabilization of distinct receptor conformations by individual ligands. These distinct conformations control subsequent recruitment of transducer and effector proteins. Here, we report that ligand efficacy ...
DOI:
10.1016/j.cell.2016.09.021

2. The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

Author:
Wootten, Denise; Reynolds, Christopher A.; Smith, Kevin J.; Mobarec, Juan C.; Koole, Cassandra; Savage, Emilia E.; Pabreja, Kavita; Simms, John; Sridhar, Rohan; Furness, Sebastian G.B.; Liu, Mengjie; Thompson, Philip E.; Miller, Laurence J.; Christopoulos, Arthur; Sexton, Patrick M.
Source:
Cell 2016 v.165 pp. 1632-1643
ISSN:
0092-8674
Subject:
G-protein coupled receptors,   etc   ; agonists; analytical methods; glucagon-like peptide 1; ligands; models; therapeutics;     Show all 7 Subjects
Abstract:
... Ligand-directed signal bias offers opportunities for sculpting molecular events, with the promise of better, safer therapeutics. Critical to the exploitation of signal bias is an understanding of the molecular events coupling ligand binding to intracellular signaling. Activation of class B G protein-coupled receptors is driven by interaction of the peptide N terminus with the receptor core. To und ...
DOI:
10.1016/j.cell.2016.05.023
PubMed:
27315480
PubMed Central:
PMC4912689