This proposal requests support for a Keystone Symposia meeting entitled G Protein-Coupled Receptors: Molecular Mechanisms and Novel Functional Insights, organized by Arthur Christopoulos and Michel Bouvier, which will be held in Alberta, Canada from February 17 - 22, 2012. The seven transmembrane-spanning G protein-coupled receptors (GPCRs) are the largest superfamily of receptors in the human genome, are involved in virtually all physiological processes, and represent the targets for at least 30% of all current medicines. Recent years have witnessed the coalescing of a number of important paradigms, including ligand- biased signalling, allosteric modulation and receptor dimerization, with substantial advances in structural determination, chemical biology and in vivo approaches to studying GPCR function. These developments will undoubtedly have a profound impact on future approaches to GPCR-based drug discovery. This meeting will focus on the interplay between these developments, and how they can be exploited to advance the translational application of cutting-edge GPCR-based research. PUBLIC HEALTH RELEVANCE: G protein-coupled receptors (GPCRs) constitute the largest family of membrane proteins in the human genome, and include many potential therapeutic targets for a broad range of diseases such as neuropsychiatric and behavioral disorders, diabetes and obesity, cardiovascular disease, inflammation and cancer. The Keystone Symposia meeting on G Protein-Coupled Receptors: Molecular Mechanisms and Novel Functional Insights will provide a unique opportunity for scientists from diverse backgrounds to better understand the challenges of GPCR drug discovery from new perspectives and explore new approaches to more efficiently develop effective GPCR therapeutics.
NIH ExPorter
NIH ExPorter