This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
6e5v
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 6e5v is ON HOLD Authors: Chen, Q., Ho, J.D., Ashok, S., Vargas, M.C., Wang, J., Atwell, S., Bures, M., Schkeryantz, J.M., Monn, J.A., Hao, J. Descr...) |
|||
| (4 intermediate revisions not shown.) | |||
| Line 1: | Line 1: | ||
| - | '''Unreleased structure''' | ||
| - | + | ==human mGlu8 receptor amino terminal domain in complex with (S)-3,4-Dicarboxyphenylglycine (DCPG)== | |
| + | <StructureSection load='6e5v' size='340' side='right'caption='[[6e5v]], [[Resolution|resolution]] 2.95Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6e5v]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6E5V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6E5V 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]] 2.95Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=HVG:4-[(S)-amino(carboxy)methyl]benzene-1,2-dicarboxylic+acid'>HVG</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=6e5v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e5v OCA], [https://pdbe.org/6e5v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6e5v RCSB], [https://www.ebi.ac.uk/pdbsum/6e5v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6e5v ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/GRM8_HUMAN GRM8_HUMAN] G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.<ref>PMID:9473604</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | (S)-3,4-dicarboxyphenylglycine (DCPG) was first reported in 2001 as a potent orthosteric agonist with high subtype selectivity for the mGlu8 receptor, but the structural basis for its high selectivity is not well understood. We have solved a co-crystal structure of recombinant human mGlu8 amino terminal domain (ATD) protein bound to (S)-DCPG, which possesses the largest lobe opening angle observed to date among known agonist-bound mGlu ATD crystal structures. The binding conformation of (S)-DCPG observed in the crystal structure is significantly different from that in the homology model built from an L-Glutamate-bound rat mGlu1 ATD crystal structure, which has a smaller lobe opening angle. This highlights the importance of considering various lobe opening angles when modeling mGlu ATD-ligand complex. New homology models of other mGlu receptors based on the (S)-DCPG-bound mGlu8 ATD crystal structure were explored to rationalize (S)-DCPG's high mGlu8 receptor subtype selectivity. | ||
| - | + | Structural Basis for (S)-3,4-Dicarboxyphenylglycine (DCPG) As a Potent and Subtype Selective Agonist of the mGlu8 Receptor.,Chen Q, Ho JD, Ashok S, Vargas MC, Wang J, Atwell S, Bures M, Schkeryantz JM, Monn JA, Hao J J Med Chem. 2018 Oct 26. doi: 10.1021/acs.jmedchem.8b01120. PMID:30365309<ref>PMID:30365309</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[ | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 6e5v" style="background-color:#fffaf0;"></div> |
| - | [[Category: | + | |
| - | [[Category: Ashok | + | ==See Also== |
| - | [[Category: Atwell | + | *[[Metabotropic glutamate receptor 3D structures|Metabotropic glutamate receptor 3D structures]] |
| - | [[Category: Bures | + | == References == |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Wang | + | [[Category: Large Structures]] |
| + | [[Category: Ashok S]] | ||
| + | [[Category: Atwell S]] | ||
| + | [[Category: Bures M]] | ||
| + | [[Category: Chen Q]] | ||
| + | [[Category: Hao J]] | ||
| + | [[Category: Ho JD]] | ||
| + | [[Category: Monn JA]] | ||
| + | [[Category: Schkeryantz JM]] | ||
| + | [[Category: Vargas MC]] | ||
| + | [[Category: Wang J]] | ||
Current revision
human mGlu8 receptor amino terminal domain in complex with (S)-3,4-Dicarboxyphenylglycine (DCPG)
| |||||||||||
Categories: Homo sapiens | Large Structures | Ashok S | Atwell S | Bures M | Chen Q | Hao J | Ho JD | Monn JA | Schkeryantz JM | Vargas MC | Wang J
