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Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects. Here, we present a direct way to quantify the efficacy of ligands by measuring the bi...

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Detalles Bibliográficos
Autores principales: Livingston, Kathryn E, Mahoney, Jacob P, Manglik, Aashish, Sunahara, Roger K, Traynor, John R
Formato: Online Artículo Texto
Lenguaje:English
Publicado: eLife Sciences Publications, Ltd 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6042960/
https://www.ncbi.nlm.nih.gov/pubmed/29932421
http://dx.doi.org/10.7554/eLife.32499