Franziska M Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular

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

To achieve this, the work of Heydenreich et al. (2023) will be analysed to demonstrate how mutagenesis www.ecosystem.drgpcr.com/post/decoding-gpcr-function-the-role-of-mutagenesis-in-rational-drug-discovery Heydenreich M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. M. (2023). Howard, M. K., Hoppe, N., Huang, X. P., Macdonald, C. B., Mehrota, E., Grimes, P.

For instance, Heydenreich et al. (2023) developed a data science framework that combined mutagenesis Heydenreich, F. M., Marti-Solano, M., Sandhu, M., Kobilka, B. K., Bouvier, M., & Babu, M. Kosar, M., Sarott, R. C., Sykes, D. A., Viray, A. E., Vitale, R. M., Tomašević, N., ... & Carreira, E. M. (2024). M., Christopoulos, A., & May, L. T. (2016).

Magdalena M Scharf, Antonella Di Pizio, Ines Liebscher, Hannes Schihada, and Gunnar Schulte et al. on Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi and Michel Bouvier.

Nayara Braga Emidio, Ross Cheloha, Laura M Wingler, et al. for their work on Nanobody-Mediated Dualsteric Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, and Michel Bouvier.

Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier

Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier

Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, and Michel Bouvier We will also have a poster

Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier

Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, and Michel Bouvier.

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Galien Foundation Announces 2023 Prix Galien UK Award Candidates Exscientia Appoints Harvard Professor Franziska

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50% displacement threshold and progressed to seven-point concentration–response assays (10⁻¹⁰ to 10⁻⁶ M) Table reporting the % of displacement measured at 1 µ M and the corresponding Ki for those showing a Hoechst-stained nuclei (blue) across increasing concentrations of AAN396, AAN397 and AAN405 (10⁻¹⁰ to 10⁻⁶ M)

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The fission yeast Schizosaccharomyces pombe has two mating types, Plus (P) and Minus (M). investigated the stringency of the two GPCRs, Mam2 and Map3, for their respective pheromones, P-factor and M-factor acid residues of Map3, F214 and F215, are key residues important for discrimination of closely related M-factors