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Thompson , David Reiner-Link , Alessandro Berghella , Brinda K Rana , G Enrico Rovati , Valerie Capra , Caroline M Gorvin , Alexander S Hauser Calcineurin-fusion facilitates cryo-EM structure determination of a Family Abigail Alwin , Campbell Krusemark , Ezequiel Marron Fernandez de Velasco , Steven H Olson , Lauren M

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially by eliciting different levels of recruitment of effector proteins. As activation and recruitment of effector proteins might influence each other, thorough analysis of bias is difficult. Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well as arrestin3 binding to the muscarinic acetylcholine receptor M3 by utilizing FRET-based assays. In order to avoid interference between these interactions, we studied GRK2 binding in the presence of inhibitors of Gi and Gq proteins and analyzed arrestin3 binding to prestimulated M3 receptors to avoid differences in receptor phosphorylation influencing arrestin recruitment. We measured substantial differences in the agonist efficacies to induce M3R-arrestin3 versus M3R-GRK2 interaction. However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements for arrestin3 binding to M3R are distinct. Read full article

M.; Compton, D. R.; Martin, B. R.; Abood, M. E. , M. C.; Westphal, M. V.; Mostinski, Y.; Mach, L.; Wasinska-Kalwa, M.; Weise, M.; Hoare, B. .; Maccarrone, M.; Veprintsev, D. B.; Carreira, E. M.; Grether, U.; Nazaré, M. F.; Nicolotti, O.; Perrone, M. G.; Brea, J.; Loza, M. I.; Infantino, V.; Abate, C.; Contino, M.

Caroline Gorvin "Dr. Caroline Gorvin is a Wellcome Trust & Royal Society Sir Henry Dale Fellow at the Institute of Metabolism Caroline continued to undertake postdoctoral research in Oxford, investigating the signalling and trafficking Caroline moved to the University of Birmingham in 2018 to establish her research group investigating Caroline Gorvin on the web University of Birmingham Endocrine Metabolic GPCRs Society of Endocrinology

Lauren M. Slosky About Dr. Lauren M. Caron at Duke University. Dr. Lauren M.

Kathleen Caron About Kathleen M. Caron Kathleen M. Caron, Ph.D. is the Frederik L. Caron received a BS in Biology and BA in Philosophy at Emory University and a PhD at Duke University Caron has received numerous awards including a Burroughs Wellcome Fund Career Award in the Biomedical Caron currently holds multiple scientific advisory roles in academia, industry and the National Institutes Kathleen M. Caron on the web Lab Website Twitter Pubmed Google Scholar Orcid Enjoying the Dr.