The curriculum is divided into four modules, each focusing on essential aspects of pharmacological principles

Burger , Arthur Christopoulos , David M. Thal , et al., for their groundbreaking work on Positive allosteric modulation of a GPCR ternary complex

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

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David Sykes About Dr. David Sykes " David Andrew Sykes, BSc Hons Pharmacology, MSc Molecular Biology and Biochemistry, PhD David has over 20+ years of experience working in a drug discovery environment mainly in a specialist In 2014 David joined the University of Nottingham and began a part-time PhD in Molecular Pharmacology David Sykes on the web Veprintsev Lab ResearchGate LinkedIn Dr.

Davide Calebiro About Dr. Davide Calebiro "Davide Calebiro is Chair of Molecular Endocrinology and Wellcome Trust Senior Research Davide’s work has been published in prestigious scientific journals such as Nature, Cell, New England Davide Calebiro on the web University of Birmingham Twitter Google Scholar LinkedIn Dr.

David E. Gloriam About this episode David Gloriam is a Professor in Computational Receptor Biology at the University David obtained his Ph.D. from Uppsala University in Sweden where he worked on the bioinformatic identification Join me a learn more about David’s work, his career trajectory, and GPCRdb. Dr. David E.