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

  title={Allosteric coupling from G protein to the agonist binding pocket in GPCRs},
  author={Brian T. DeVree and Jacob P. Mahoney and Gisselle A. V{\'e}lez-Ruiz and Soren G. F. Rasmussen and Adam J. Kuszak and Elin Edwald and Juan-Jose Fung and Aashish Manglik and Matthieu Masureel and Yang Du and Rachel A Matt and Els Pardon and Jan Steyaert and Brian K. Kobilka and Roger K Sunahara},
G-protein-coupled receptors (GPCRs) remain the primary conduit by which cells detect environmental stimuli and communicate with each other. Upon activation by extracellular agonists, these seven-transmembrane-domain-containing receptors interact with heterotrimeric G proteins to regulate downstream second messenger and/or protein kinase cascades. Crystallographic evidence from a prototypic GPCR, the β2-adrenergic receptor (β2AR), in complex with its cognate G protein, Gs, has provided a model… CONTINUE READING
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