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- 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
- Cell 2016 v.167 pp. 739-749.e11
- G-protein coupled receptors, etc ; agonists; calcitonin; drugs; guanosine triphosphate; ligands; protein conformation; second messengers; Show all 8 Subjects
- ... 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 ...
- 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.
- Cell 2016 v.165 pp. 1632-1643
- G-protein coupled receptors, etc ; agonists; analytical methods; glucagon-like peptide 1; ligands; models; therapeutics; Show all 7 Subjects
- ... 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 ...
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