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Specific Engineered G Protein Coupling to Histamine Receptors Revealed from Cellular Assay Experiments and Accelerated Molecular Dynamics Simulations

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Höring, Carina ; Conrad, Marcus ; Söldner, Christian A. ; Wang, Jinan ; Sticht, Heinrich ; Strasser, Andrea ; Miao, Yinglong
License: Creative Commons Attribution 4.0
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Date of publication of this fulltext: 12 Jan 2022 11:05


G protein-coupled receptors (GPCRs) are targets of extracellular stimuli and hence occupy a key position in drug discovery. By specific and not yet fully elucidated coupling profiles with alpha subunits of distinct G protein families, they regulate cellular responses. The histamine H-2 and H-4 receptors (H2R and H4R) are prominent members of Gs- and Gi-coupled GPCRs. Nevertheless, promiscuous G ...


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