5nx2
From Proteopedia
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(New page: '''Unreleased structure''' The entry 5nx2 is ON HOLD Authors: Rappas, M., Jazayeri, A., Brown, A.J.H., Kean, J., Errey, J.C., Robertson, N., Fiez-Vandal, C., Andrews, S.P., Congreve, M....) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of thermostabilised full-length GLP-1R in complex with a truncated peptide agonist at 3.7 A resolution== | |
| + | <StructureSection load='5nx2' size='340' side='right'caption='[[5nx2]], [[Resolution|resolution]] 3.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5nx2]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NX2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5NX2 FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.7Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9DK:3-[2-(1~{H}-imidazol-4-yl)ethylamino]-2,2-dimethyl-3-oxidanylidene-propanoic+acid'>9DK</scene>, <scene name='pdbligand=9DQ:(2~{S})-2-azanyl-3-(1~{H}-1,2,3,4-tetrazol-5-yl)propanoic+acid'>9DQ</scene>, <scene name='pdbligand=9DT:(2~{S})-2-azanyl-3-(2-fluorophenyl)-2-methyl-propanoic+acid'>9DT</scene>, <scene name='pdbligand=9DW:(2~{S})-2-azanyl-3-[4-(2-ethyl-4-methoxy-phenyl)phenyl]propanoic+acid'>9DW</scene>, <scene name='pdbligand=9DZ:(2~{S})-2-azanyl-5-(3,5-dimethylphenyl)pentanamide'>9DZ</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=SOG:2-HYDROXYMETHYL-6-OCTYLSULFANYL-TETRAHYDRO-PYRAN-3,4,5-TRIOL'>SOG</scene></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=5nx2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nx2 OCA], [https://pdbe.org/5nx2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5nx2 RCSB], [https://www.ebi.ac.uk/pdbsum/5nx2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5nx2 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/GLP1R_HUMAN GLP1R_HUMAN] This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Glucagon-like peptide 1 (GLP-1) regulates glucose homeostasis through the control of insulin release from the pancreas. GLP-1 peptide agonists are efficacious drugs for the treatment of diabetes. To gain insight into the molecular mechanism of action of GLP-1 peptides, here we report the crystal structure of the full-length GLP-1 receptor bound to a truncated peptide agonist. The peptide agonist retains an alpha-helical conformation as it sits deep within the receptor-binding pocket. The arrangement of the transmembrane helices reveals hallmarks of an active conformation similar to that observed in class A receptors. Guided by this structural information, we design peptide agonists with potent in vivo activity in a mouse model of diabetes. | ||
| - | + | Crystal structure of the GLP-1 receptor bound to a peptide agonist.,Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Dore AS, Weir M, Cooke RM, Marshall FH Nature. 2017 Jun 8;546(7657):254-258. doi: 10.1038/nature22800. Epub 2017 May 31. PMID:28562585<ref>PMID:28562585</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 5nx2" style="background-color:#fffaf0;"></div> |
| - | [[Category: | + | |
| - | [[Category: Baig | + | ==See Also== |
| - | [[Category: | + | *[[Glucagon-like peptide receptor 3D structures|Glucagon-like peptide receptor 3D structures]] |
| - | [[Category: | + | == References == |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Fiez-Vandal | + | [[Category: Large Structures]] |
| - | [[Category: Kean | + | [[Category: Synthetic construct]] |
| - | [[Category: Marshall | + | [[Category: Andrews SP]] |
| - | [[Category: | + | [[Category: Baig AH]] |
| - | [[Category: | + | [[Category: Bortolato A]] |
| - | [[Category: | + | [[Category: Brown AJH]] |
| - | [[Category: | + | [[Category: Congreve M]] |
| - | [[Category: | + | [[Category: Cooke RM]] |
| + | [[Category: Dore AS]] | ||
| + | [[Category: Errey JC]] | ||
| + | [[Category: Fiez-Vandal C]] | ||
| + | [[Category: Jazayeri A]] | ||
| + | [[Category: Kean J]] | ||
| + | [[Category: Marshall FH]] | ||
| + | [[Category: Mason JS]] | ||
| + | [[Category: Rappas M]] | ||
| + | [[Category: Robertson N]] | ||
| + | [[Category: Teobald I]] | ||
| + | [[Category: Weir M]] | ||
Current revision
Crystal structure of thermostabilised full-length GLP-1R in complex with a truncated peptide agonist at 3.7 A resolution
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Categories: Homo sapiens | Large Structures | Synthetic construct | Andrews SP | Baig AH | Bortolato A | Brown AJH | Congreve M | Cooke RM | Dore AS | Errey JC | Fiez-Vandal C | Jazayeri A | Kean J | Marshall FH | Mason JS | Rappas M | Robertson N | Teobald I | Weir M
