GPCR Network: a large-scale collaboration on GPCR structure and function
By Raymond C. Stevens, Vadim Cherezov, Vsevolod Katritch, Ruben Abagyan, P. Kuhn, H. Rosen, Kurt Wüthrich. Nature reviews. Drug discovery, 2012
303 citations recorded by the source corpus.
G protein-coupled receptors (GPCRs) are targeted by ∼30–40% of marketed drugs, and their key roles in normal physiology and in disease demonstrate that an understanding of their structure and function is valuable to researchers in both basic science and drug discovery. However, until recently, detailed structural information on this protein family was limited by challenges in X-ray crystallographic analysis of such membrane proteins. The GPCR Network was created in 2010 with the goal of structurally characterizing 15–25 representative human GPCRs within 5 years, based on an active outreach programme addressing an interdisciplinary community of scientists interested in GPCR structure, chemistry and biology. Here, we provide an overview of how this collaborative effort has enabled the structural determination and characterization of eight human GPCRs so far, and discuss some of the challenges that remain in gaining more detailed insights into structure–function relationships in this receptor superfamily.
Subfields: Cellular and Molecular Neuroscience, Computational Theory and Mathematics, Molecular Biology
View Paper: https://www.semanticscholar.org/paper/b7fa63eaf43f0df5829742ba0ffaccaff32cd360
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Citations in the corpus
- A Structural Framework for GPCR Chemogenomics: What's In a Residue Number? (2018, background): “Upon binding these molecules from the extracellular space, a signal is relayed to the intracellular space by activating various signaling pathways [1, 2].”