5nx2

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m (Protected "5nx2" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 5nx2 is ON HOLD
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==Crystal structure of thermostabilised full-length GLP-1R in complex with a truncated peptide agonist at 3.7 A resolution==
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<StructureSection load='5nx2' size='340' side='right' caption='[[5nx2]], [[Resolution|resolution]] 3.70&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5nx2]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. 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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5NX2 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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>
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<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=9DK:'>9DK</scene>, <scene name='pdbligand=9DQ:'>9DQ</scene>, <scene name='pdbligand=9DT:'>9DT</scene>, <scene name='pdbligand=9DW:'>9DW</scene>, <scene name='pdbligand=9DZ:'>9DZ</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GLP1R ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5nx2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nx2 OCA], [http://pdbe.org/5nx2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5nx2 RCSB], [http://www.ebi.ac.uk/pdbsum/5nx2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5nx2 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://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.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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.
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Authors: Rappas, M., Jazayeri, A., Brown, A.J.H., Kean, J., Errey, J.C., Robertson, N., Fiez-Vandal, C., Andrews, S.P., Congreve, M., Bortolato, A., Mason, J.S., Baig, A.H., Teobald, I., Dore, A.S., Weir, M., Cooke, R.M., Marshall, F.H.
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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>
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Description: Crystal structure of thermostabilised full-length GLP-1R in complex with a truncated peptide agonist at 3.7 A resolution
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Andrews, S.P]]
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<div class="pdbe-citations 5nx2" style="background-color:#fffaf0;"></div>
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[[Category: Brown, A.J.H]]
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== References ==
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[[Category: Baig, A.H]]
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<references/>
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[[Category: Weir, M]]
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__TOC__
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[[Category: Congreve, M]]
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</StructureSection>
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[[Category: Mason, J.S]]
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[[Category: Human]]
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[[Category: Jazayeri, A]]
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[[Category: Andrews, S P]]
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[[Category: Robertson, N]]
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[[Category: Baig, A H]]
[[Category: Bortolato, A]]
[[Category: Bortolato, A]]
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[[Category: Brown, A J.H]]
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[[Category: Congreve, M]]
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[[Category: Cooke, R M]]
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[[Category: Dore, A S]]
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[[Category: Errey, J C]]
[[Category: Fiez-Vandal, C]]
[[Category: Fiez-Vandal, C]]
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[[Category: Jazayeri, A]]
[[Category: Kean, J]]
[[Category: Kean, J]]
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[[Category: Marshall, F.H]]
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[[Category: Marshall, F H]]
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[[Category: Cooke, R.M]]
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[[Category: Mason, J S]]
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[[Category: Errey, J.C]]
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[[Category: Teobald, I]]
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[[Category: Rappas, M]]
[[Category: Rappas, M]]
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[[Category: Dore, A.S]]
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[[Category: Robertson, N]]
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[[Category: Teobald, I]]
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[[Category: Weir, M]]
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[[Category: Gpcr]]
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[[Category: Membrane protein]]
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[[Category: Signalling protein]]

Revision as of 09:56, 16 November 2017

Crystal structure of thermostabilised full-length GLP-1R in complex with a truncated peptide agonist at 3.7 A resolution

5nx2, resolution 3.70Å

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