3pbl
From Proteopedia
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| - | {{STRUCTURE_3pbl| PDB=3pbl | SCENE= }} | ||
| - | ===Structure of the human dopamine D3 receptor in complex with eticlopride=== | ||
| - | {{ABSTRACT_PUBMED_21097933}} | ||
| - | == | + | ==Structure of the human dopamine D3 receptor in complex with eticlopride== |
| - | [[3pbl]] is a 2 chain structure with sequence from [ | + | <StructureSection load='3pbl' size='340' side='right'caption='[[3pbl]], [[Resolution|resolution]] 2.89Å' scene=''> |
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3pbl]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_virus_T4 Escherichia virus T4] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PBL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PBL 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]] 2.89Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ETQ:3-CHLORO-5-ETHYL-N-{[(2S)-1-ETHYLPYRROLIDIN-2-YL]METHYL}-6-HYDROXY-2-METHOXYBENZAMIDE'>ETQ</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=PRD_900001:alpha-maltose'>PRD_900001</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=3pbl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pbl OCA], [https://pdbe.org/3pbl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pbl RCSB], [https://www.ebi.ac.uk/pdbsum/3pbl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pbl ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [https://www.uniprot.org/uniprot/DRD3_HUMAN DRD3_HUMAN] Hereditary essential tremor. Disease susceptibility is associated with variations affecting the gene represented in this entry. | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/ENLYS_BPT4 ENLYS_BPT4] Endolysin with lysozyme activity that degrades host peptidoglycans and participates with the holin and spanin proteins in the sequential events which lead to the programmed host cell lysis releasing the mature viral particles. Once the holin has permeabilized the host cell membrane, the endolysin can reach the periplasm and break down the peptidoglycan layer.<ref>PMID:22389108</ref> [https://www.uniprot.org/uniprot/DRD3_HUMAN DRD3_HUMAN] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.<ref>PMID:19520868</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Dopamine modulates movement, cognition, and emotion through activation of dopamine G protein-coupled receptors in the brain. The crystal structure of the human dopamine D3 receptor (D3R) in complex with the small molecule D2R/D3R-specific antagonist eticlopride reveals important features of the ligand binding pocket and extracellular loops. On the intracellular side of the receptor, a locked conformation of the ionic lock and two distinctly different conformations of intracellular loop 2 are observed. Docking of R-22, a D3R-selective antagonist, reveals an extracellular extension of the eticlopride binding site that comprises a second binding pocket for the aryl amide of R-22, which differs between the highly homologous D2R and D3R. This difference provides direction to the design of D3R-selective agents for treating drug abuse and other neuropsychiatric indications. | ||
| - | + | Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.,Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC Science. 2010 Nov 19;330(6007):1091-5. PMID:21097933<ref>PMID:21097933</ref> | |
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| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | < | + | </div> |
| - | + | <div class="pdbe-citations 3pbl" style="background-color:#fffaf0;"></div> | |
| - | [[ | + | |
| - | [[ | + | ==See Also== |
| - | [[ | + | *[[Dopamine receptor|Dopamine receptor]] |
| - | [[ | + | *[[Dopamine receptor 3D structures|Dopamine receptor 3D structures]] |
| - | + | *[[Lysozyme 3D structures|Lysozyme 3D structures]] | |
| - | + | *[[Neurotransmitters|Neurotransmitters]] | |
| - | + | == References == | |
| - | + | <references/> | |
| - | [[Category: | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: | + | [[Category: Escherichia virus T4]] |
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Cherezov V]] |
| - | [[Category: | + | [[Category: Chien EYT]] |
| - | [[Category: | + | [[Category: Han GW]] |
| - | [[Category: | + | [[Category: Katritch V]] |
| - | [[Category: | + | [[Category: Liu W]] |
| - | + | [[Category: Stevens RC]] | |
| - | + | [[Category: Zhao Q]] | |
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Current revision
Structure of the human dopamine D3 receptor in complex with eticlopride
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Categories: Escherichia virus T4 | Homo sapiens | Large Structures | Cherezov V | Chien EYT | Han GW | Katritch V | Liu W | Stevens RC | Zhao Q
