7yfd

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Current revision (09:22, 17 October 2024) (edit) (undo)
 
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7yfd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7yfd OCA], [https://pdbe.org/7yfd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7yfd RCSB], [https://www.ebi.ac.uk/pdbsum/7yfd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7yfd ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7yfd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7yfd OCA], [https://pdbe.org/7yfd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7yfd RCSB], [https://www.ebi.ac.uk/pdbsum/7yfd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7yfd ProSAT]</span></td></tr>
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== Function ==
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<div style="background-color:#fffaf0;">
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[https://www.uniprot.org/uniprot/GBB1_HUMAN GBB1_HUMAN] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.<ref>PMID:18611381</ref>
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== Publication Abstract from PubMed ==
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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.
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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<ref>PMID:37863901</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 7yfd" style="background-color:#fffaf0;"></div>
==See Also==
==See Also==
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[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Mus musculus]]
[[Category: Mus musculus]]
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[[Category: Dohyun I]]
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[[Category: Asada H]]
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[[Category: Hidetsugu A]]
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[[Category: Im D]]
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[[Category: So I]]
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[[Category: Iwata S]]

Current revision

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

PDB ID 7yfd

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