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| - | | + | #REDIRECT [[6cm4]] This PDB entry is obsolete and replaced by 6cm4 |
| - | ==Structure of the D2 Dopamine Receptor Bound to the Atypical Antipsychotic Drug Risperidone==
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| - | <StructureSection load='6c38' size='340' side='right' caption='[[6c38]], [[Resolution|resolution]] 2.87Å' scene=''>
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| - | == Structural highlights ==
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| - | <table><tr><td colspan='2'>[[6c38]] is a 1 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=6C38 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6C38 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=8NU:3-[2-[4-(6-fluoranyl-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one'>8NU</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene></td></tr>
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| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">DRD2 ([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='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></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=6c38 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6c38 OCA], [http://pdbe.org/6c38 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6c38 RCSB], [http://www.ebi.ac.uk/pdbsum/6c38 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6c38 ProSAT]</span></td></tr>
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| - | </table>
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| - | == Disease ==
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| - | [[http://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Myoclonic dystonia 11. The gene represented in this entry may be involved in disease pathogenesis. DRD2 mutations in myoclonic dystonia patients are rare, and their contribution to disease phenotype is unclear (PubMed:10716258).
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| - | == Function ==
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| - | [[http://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (By similarity).<ref>PMID:21645528</ref> <ref>PMID:17264214</ref>
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| - | <div style="background-color:#fffaf0;">
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| - | == Publication Abstract from PubMed ==
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| - | Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward, addiction, control of coordinated movement, metabolism and hormonal secretion. Correspondingly, dysregulation of the dopaminergic system has been implicated in diseases such as schizophrenia, Parkinson's disease, depression, attention deficit hyperactivity disorder, nausea and vomiting, among others. Dopamine's actions are mediated by a family of five G-protein coupled receptors (GPCRs) (viz. D1, D2, D3, D4 and D5)(1). The D2 dopamine receptor (DRD2) is the primary target for both typical(2) and atypical(3,4) antipsychotic drugs, and for Parkinson's disease drugs. Unfortunately, many drugs targeting DRD2 frequently cause serious and potentially life-threatening side effects due to promiscuous activities against related receptors(4,5). Accordingly, a molecular understanding of DRD2 structure and function could provide a template for the design of safer and more effective medications. Here we provide the crystal structure of DRD2 in complex with the widely prescribed atypical antipsychotic drug risperidone. The DRD2-risperidone structure reveals an unexpected mode of antipsychotic drug binding to dopamine receptors, and illuminates structural determinants essential for the actions of risperidone and related drugs at DRD2.
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| - | Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone.,Wang S, Che T, Levit A, Shoichet BK, Wacker D, Roth BL Nature. 2018 Jan 24. pii: nature25758. doi: 10.1038/nature25758. PMID:29466326<ref>PMID:29466326</ref>
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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| - | </div>
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| - | <div class="pdbe-citations 6c38" style="background-color:#fffaf0;"></div>
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| - | == References ==
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| - | <references/>
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| - | __TOC__
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| - | </StructureSection>
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| - | [[Category: Human]]
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| - | [[Category: Lysozyme]]
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| - | [[Category: Che, T]]
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| - | [[Category: Levit, A]]
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| - | [[Category: Roth, B L]]
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| - | [[Category: Shoichet, B K]]
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| - | [[Category: Wacker, D]]
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| - | [[Category: Wang, S]]
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| - | [[Category: Antipsychotic]]
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| - | [[Category: D2]]
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| - | [[Category: Dopamine receptor]]
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| - | [[Category: Gpcr]]
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| - | [[Category: Membrane protein]]
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| - | [[Category: Risperidone]]
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