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The European Research Network on Signal Transduction (ERNEST): toward a multidimensional holistic understanding of G protein-coupled receptor signaling

Item Type:Review
Title:The European Research Network on Signal Transduction (ERNEST): toward a multidimensional holistic understanding of G protein-coupled receptor signaling
Creators Name:Sommer, M.E., Selent, J., Carlsson, J., De Graaf, C., Gloriam, D.E., Keseru, G.M., Kosloff, M., Mordalski, S., Rizk, A., Rosenkilde, M.M., Sotelo, E., Tiemann, J.K.S., Tobin, A., Vardjan, N., Waldhoer, M. and Kolb, P.
Abstract:G protein-coupled receptors (GPCRs) are intensively studied due to their therapeutic potential as drug targets. Members of this large family of transmembrane receptor proteins mediate signal transduction in diverse cell types and play key roles in human physiology and health. In 2013 the research consortium GLISTEN (COST Action CM1207) was founded with the goal of harnessing the substantial growth in knowledge of GPCR structure and dynamics to push forward the development of molecular modulators of GPCR function. The success of GLISTEN, coupled with new findings and paradigm shifts in the field, led in 2019 to the creation of a related consortium called ERNEST (COST Action CA18133). ERNEST broadens focus to entire signaling cascades, based on emerging ideas of how complexity and specificity in signal transduction are not determined by receptor-ligand interactions alone. A holistic approach that unites the diverse data and perspectives of the research community into a single multidimensional map holds great promise for improved drug design and therapeutic targeting.
Keywords:G Protein-Coupled Receptor, GPCR, Signal Transduction, Biased Agonism, Functional Selectivity, Structure Based Drug Design
Source:ACS Pharmacology & Translational Science
ISSN:2575-9108
Publisher:American Chemical Society
Volume:3
Number:2
Page Range:361-370
Date:10 April 2020
Additional Information:Copyright © 2020 American Chemical Society
Official Publication:https://doi.org/10.1021/acsptsci.0c00024
External Fulltext:View full text on PubMed Central
PubMed:View item in PubMed

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