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surprising discovery that β-arrestin can bind GPCRs without receptor activation, to visualizing intermediate states the Symposia GPCR Publication Highlights     Arrestin recognizes GPCRs independently of the receptor state Triple Labeling Resolves a GPCR Intermediate State by Using Three-Color Single Molecule FRET .   A powerful three-color approach captures dynamic receptor states in real time. Whether you're decoding a hidden receptor state or hunting for the next orphan GPCR ligand, we're here

Why the Myth of High and Low Affinity Binding Sites Could Be Slowing Your Pipeline   If you’re working The interpretation of high and low affinity binding sites  on GPCRs.   appears to bind at two different affinities in the same system, it seems logical to assume two distinct sites But are these differences really pointing to two physical sites?   formation of ligand-receptor-G protein complexes —an observation that creates the illusion of multiple sites

Exploring the intracellular allosteric site GPCRs represent one of the largest and most vital families distinct, often less conserved sites on the receptor. overlap with) the orthosteric site (Rosenbaum, Rasmussen et al. 2009). Advantages of targeting GPCRs allosteric sites Allosteric sites offer a more nuanced approach to modulating Allosteric agonists binding to intracellular sites can also promote G-protein signaling.

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Home → Flash News → A large-scale analysis of GPCR molecular dynamics reveals hidden allosteric sites structural-and-molecular-insights-into-gpcr-function/large-scale-investigation-of-gpcr-molecular-dynamics-data-uncovers-allosteric-sites-and-lateral-gateways Category GPCR Weekly News A large-scale analysis of GPCR molecular dynamics reveals hidden allosteric sites structural-and-molecular-insights-into-gpcr-function/large-scale-investigation-of-gpcr-molecular-dynamics-data-uncovers-allosteric-sites-and-lateral-gateways