Allosteric coupling from G protein to the agonist-binding pocket in GPCRs

Brian T. DeVree, Jacob P. Mahoney, Gisselle A. Vélez-Ruiz, Soren G. F. Rasmussen, Adam J. Kuszak, Elin Edwald, Juan-Jose Fung, Aashish Manglik, Matthieu Masureel, Yang Du, Rachel A. Matt, Els Pardon, Jan Steyaert, Brian K. Kobilka and Roger K. Sunahara ()
Additional contact information
Brian T. DeVree: University of Michigan Medical School
Jacob P. Mahoney: University of Michigan Medical School
Gisselle A. Vélez-Ruiz: University of Michigan Medical School
Soren G. F. Rasmussen: Stanford University
Adam J. Kuszak: University of Michigan Medical School
Elin Edwald: University of Michigan Medical School
Juan-Jose Fung: Stanford University
Aashish Manglik: Stanford University
Matthieu Masureel: Stanford University
Yang Du: Stanford University
Rachel A. Matt: Stanford University
Els Pardon: Structural Biology Research Center, VIB, Vrije Universiteit Brussel (VUB)
Jan Steyaert: Structural Biology Brussels, Vrije Universiteit Brussel (VUB)
Brian K. Kobilka: Stanford University
Roger K. Sunahara: University of Michigan Medical School

Nature, 2016, vol. 535, issue 7610, 182-186

Abstract: Here, pharmacological and biochemical evidence is provided that shows that G-protein coupling to the β2-adrenergic receptor stabilizes a ‘closed’ conformation of the G-protein-coupled receptor (GPCR) and that that the effects of the G protein on the ligand-binding site of the GPCR are observed even in the absence of a bound agonist.

Date: 2016
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DOI: 10.1038/nature18324

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