Ontology highlight
ABSTRACT:
SUBMITTER: Kahsai AW
PROVIDER: S-EPMC4990464 | biostudies-literature | 2016 Sep
REPOSITORIES: biostudies-literature
Kahsai Alem W AW Wisler James W JW Lee Jungmin J Ahn Seungkirl S Cahill Iii Thomas J TJ Dennison S Moses SM Staus Dean P DP Thomsen Alex R B AR Anasti Kara M KM Pani Biswaranjan B Wingler Laura M LM Desai Hemant H Bompiani Kristin M KM Strachan Ryan T RT Qin Xiaoxia X Alam S Munir SM Sullenger Bruce A BA Lefkowitz Robert J RJ
Nature chemical biology 20160711 9
G-protein-coupled receptor (GPCR) ligands function by stabilizing multiple, functionally distinct receptor conformations. This property underlies the ability of 'biased agonists' to activate specific subsets of a given receptor's signaling profile. However, stabilizing distinct active GPCR conformations to enable structural characterization of mechanisms underlying GPCR activation remains difficult. These challenges have accentuated the need for receptor tools that allosterically stabilize and r ...[more]