7yfd | pdb_00007yfd

Cryo-EM structure of the imetit-bound histamine H4 receptor and Gq complex

spinqualitylabelsall models 7yfd, resolution 3.10Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 7yfd is a 6 chain structure with sequence from Homo sapiens, Lama glama and Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Electron Microscopy, Resolution 3.1Å Ligands: CLR, ITF Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed Histamine is a biogenic amine that participates in allergic and inflammatory processes by stimulating histamine receptors. The histamine H(4) receptor (H(4)R) is a potential therapeutic target for chronic inflammatory diseases such as asthma and atopic dermatitis. Here, we show the cryo-electron microscopy structures of the H(4)R-G(q) complex bound with an endogenous agonist histamine or the selective agonist imetit bound in the orthosteric binding pocket. The structures demonstrate binding mode of histamine agonists and that the subtype-selective agonist binding causes conformational changes in Phe344(7.39), which, in turn, form the "aromatic slot". The results provide insights into the molecular underpinnings of the agonism of H(4)R and subtype selectivity of histamine receptors, and show that the H(4)R structures may be valuable in rational drug design of drugs targeting the H(4)R. Structural insights into the agonists binding and receptor selectivity of human histamine H(4) receptor.,Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S Nat Commun. 2023 Oct 20;14(1):6538. doi: 10.1038/s41467-023-42260-z. PMID:37863901 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Transducin 3D structures

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