2o8h

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[[Image:2o8h.gif|left|200px]]
 
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==Crystal structure of the catalytic domain of rat phosphodiesterase 10A==
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The line below this paragraph, containing "STRUCTURE_2o8h", creates the "Structure Box" on the page.
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<StructureSection load='2o8h' size='340' side='right'caption='[[2o8h]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2o8h]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2O8H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2O8H FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=227:6,7-DIMETHOXY-4-{8-[(4-METHYLPIPERAZIN-1-YL)SULFONYL]-3,4-DIHYDROISOQUINOLIN-2(1H)-YL}QUINAZOLINE'>227</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_2o8h| PDB=2o8h | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2o8h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2o8h OCA], [https://pdbe.org/2o8h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2o8h RCSB], [https://www.ebi.ac.uk/pdbsum/2o8h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2o8h ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PDE10_RAT PDE10_RAT] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:10583409</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/o8/2o8h_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2o8h ConSurf].
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<div style="clear:both"></div>
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'''Crystal structure of the catalytic domain of rat phosphodiesterase 10A'''
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==See Also==
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*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
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== References ==
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==Overview==
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<references/>
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A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A.
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__TOC__
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</StructureSection>
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==About this Structure==
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[[Category: Large Structures]]
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2O8H is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2O8H OCA].
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==Reference==
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Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors., Chappie TA, Humphrey JM, Allen MP, Estep KG, Fox CB, Lebel LA, Liras S, Marr ES, Menniti FS, Pandit J, Schmidt CJ, Tu M, Williams RD, Yang FV, J Med Chem. 2007 Jan 25;50(2):182-5. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17228859 17228859]
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[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Single protein]]
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[[Category: Marr ES]]
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[[Category: Marr, E S.]]
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[[Category: Pandit J]]
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[[Category: Pandit, J.]]
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[[Category: Phosphodiesterase 10a]]
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[[Category: Zn-binding site]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:27:08 2008''
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Current revision

Crystal structure of the catalytic domain of rat phosphodiesterase 10A

PDB ID 2o8h

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