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site and a GPCR Paper with his team: Targeted Drug Design through GPCR Mutagenesis: Insights from β2AR China M Payne ,   Cam Sinh Lu ,   Karen Gregory ,  Lauren May ,  Andrea Vernall , et al. for their fantastic

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

February 2022 Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner by data from a Phase 3 bridging study of oliceridine injection compared to IV morphine, conducted in China success payments upon approval and commercialization milestones, as well as a 10% royalty on net sales in China commercialization of novel medicines for patients with central nervous system (CNS) disorders, today announced that China United States by the Food and Drug Administration (FDA) for use in adults for the management of acute pain

Lauren M. Slosky About Dr. Lauren M. Lauren M.

Molecular Physiology and Biophysics, Vanderbilt University, Nashville, TN 37232, USA 4 Peking University, China Hamm, Ph.D. is the Aileen M.

to cladribine, high-dose cytarabine, granulocyte colony-stimulating factor, and mitoxantrone (CLAG-M) Comparing outcomes using CLAG-M/sorafenib with those of a matched cohort of 76 patients treated with CLAG-M alone, multivariable-adjusted survival estimates were improved for 41 patients receiving CLAG-M These data suggest that CLAG-M/sorafenib is safe and improves OS and EFS relative to CLAG-M alone, with