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6e5v
From Proteopedia
(Difference between revisions)
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| - | '''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. 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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6E5V FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6e5v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e5v OCA], [http://pdbe.org/6e5v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6e5v RCSB], [http://www.ebi.ac.uk/pdbsum/6e5v PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6e5v ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://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> | |
| - | + | <div class="pdbe-citations 6e5v" style="background-color:#fffaf0;"></div> | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| + | </StructureSection> | ||
[[Category: Ashok, S]] | [[Category: Ashok, S]] | ||
| - | [[Category: Schkeryantz, J.M]] | ||
[[Category: Atwell, S]] | [[Category: Atwell, S]] | ||
| + | [[Category: Bures, M]] | ||
[[Category: Chen, Q]] | [[Category: Chen, Q]] | ||
| - | [[Category: Ho, J | + | [[Category: Hao, J]] |
| + | [[Category: Ho, J D]] | ||
| + | [[Category: Monn, J A]] | ||
| + | [[Category: Schkeryantz, J M]] | ||
| + | [[Category: Vargas, M C]] | ||
[[Category: Wang, J]] | [[Category: Wang, J]] | ||
| + | [[Category: Dcpg]] | ||
| + | [[Category: Grm8]] | ||
| + | [[Category: Mglur8 atd]] | ||
| + | [[Category: Signaling protein]] | ||
Revision as of 12:14, 7 November 2018
human mGlu8 receptor amino terminal domain in complex with (S)-3,4-Dicarboxyphenylglycine (DCPG)
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Categories: Ashok, S | Atwell, S | Bures, M | Chen, Q | Hao, J | Ho, J D | Monn, J A | Schkeryantz, J M | Vargas, M C | Wang, J | Dcpg | Grm8 | Mglur8 atd | Signaling protein
