7f8u
From Proteopedia
(Difference between revisions)
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==Crystal structure of the cholecystokinin receptor CCKAR in complex with lintitript== | ==Crystal structure of the cholecystokinin receptor CCKAR in complex with lintitript== | ||
| - | <StructureSection load='7f8u' size='340' side='right'caption='[[7f8u]]' scene=''> | + | <StructureSection load='7f8u' size='340' side='right'caption='[[7f8u]], [[Resolution|resolution]] 2.80Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7F8U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F8U FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[7f8u]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7F8U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F8U FirstGlance]. <br> |
| - | </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=7f8u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f8u OCA], [https://pdbe.org/7f8u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f8u RCSB], [https://www.ebi.ac.uk/pdbsum/7f8u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f8u ProSAT]</span></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1OE:2-[2-[[4-(2-chlorophenyl)-1,3-thiazol-2-yl]carbamoyl]indol-1-yl]ethanoic+acid'>1OE</scene></td></tr> |
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </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=7f8u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f8u OCA], [https://pdbe.org/7f8u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f8u RCSB], [https://www.ebi.ac.uk/pdbsum/7f8u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f8u ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [[https://www.uniprot.org/uniprot/CCKAR_HUMAN CCKAR_HUMAN]] Receptor for cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Cholecystokinin receptors, CCKAR and CCKBR, are important neurointestinal peptide hormone receptors and play a vital role in food intake and appetite regulation. Here, we report three crystal structures of the human CCKAR in complex with different ligands, including one peptide agonist and two small-molecule antagonists, as well as two cryo-electron microscopy structures of CCKBR-gastrin in complex with Gi2 and Gq, respectively. These structures reveal the recognition pattern of different ligand types and the molecular basis of peptide selectivity in the cholecystokinin receptor family. By comparing receptor structures in different conformational states, a stepwise activation process of cholecystokinin receptors is proposed. Combined with pharmacological data, our results provide atomic details for differential ligand recognition and receptor activation mechanisms. These insights will facilitate the discovery of potential therapeutics targeting cholecystokinin receptors. | ||
| + | |||
| + | Structures of the human cholecystokinin receptors bound to agonists and antagonists.,Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q Nat Chem Biol. 2021 Sep 23. pii: 10.1038/s41589-021-00866-8. doi:, 10.1038/s41589-021-00866-8. PMID:34556863<ref>PMID:34556863</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 7f8u" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: He C]] | + | [[Category: Lysozyme]] |
| - | [[Category: Wang M]] | + | [[Category: He, C]] |
| - | [[Category: Wu B]] | + | [[Category: Wang, M]] |
| - | [[Category: Yang D]] | + | [[Category: Wu, B]] |
| - | [[Category: Zhang X]] | + | [[Category: Yang, D]] |
| - | [[Category: Zhao Q]] | + | [[Category: Zhang, X]] |
| - | [[Category: Zhou Q]] | + | [[Category: Zhao, Q]] |
| - | [[Category: Zhu Y]] | + | [[Category: Zhou, Q]] |
| + | [[Category: Zhu, Y]] | ||
| + | [[Category: Cholecystokinin receptor cckar]] | ||
| + | [[Category: G protein-coulped receptor]] | ||
| + | [[Category: Lintitript]] | ||
| + | [[Category: Structural protein]] | ||
Revision as of 10:59, 16 February 2022
Crystal structure of the cholecystokinin receptor CCKAR in complex with lintitript
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