4dff

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==The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia==
==The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia==
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<StructureSection load='4dff' size='340' side='right' caption='[[4dff]], [[Resolution|resolution]] 2.11&Aring;' scene=''>
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<StructureSection load='4dff' size='340' side='right'caption='[[4dff]], [[Resolution|resolution]] 2.11&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4dff]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4DFF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4DFF FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4dff]] 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=4DFF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4DFF 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=0JP:8,9-DIMETHOXY-1-(1,3-THIAZOL-5-YL)-5,6-DIHYDROIMIDAZO[5,1-A]ISOQUINOLINE'>0JP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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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]] 2.11&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PDE10A ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=0JP:8,9-DIMETHOXY-1-(1,3-THIAZOL-5-YL)-5,6-DIHYDROIMIDAZO[5,1-A]ISOQUINOLINE'>0JP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></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=4dff FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4dff OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4dff RCSB], [http://www.ebi.ac.uk/pdbsum/4dff PDBsum]</span></td></tr>
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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=4dff FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4dff OCA], [https://pdbe.org/4dff PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4dff RCSB], [https://www.ebi.ac.uk/pdbsum/4dff PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4dff ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN]] 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:17389385</ref>
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[https://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN] 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:17389385</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
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<div class="pdbe-citations 4dff" style="background-color:#fffaf0;"></div>
==See Also==
==See Also==
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*[[Phosphodiesterase|Phosphodiesterase]]
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*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Bercovici, A]]
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[[Category: Large Structures]]
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[[Category: Bleichardt, C]]
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[[Category: Bercovici A]]
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[[Category: Greenlee, W J]]
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[[Category: Bleichardt C]]
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[[Category: Guzzi, M]]
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[[Category: Greenlee WJ]]
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[[Category: Ho, G D]]
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[[Category: Guzzi M]]
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[[Category: Hodgson, R]]
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[[Category: Ho GD]]
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[[Category: Hruza, A]]
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[[Category: Hodgson R]]
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[[Category: Mullins, D]]
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[[Category: Hruza A]]
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[[Category: Rijn, R Van]]
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[[Category: Mullins D]]
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[[Category: Rindgen, D]]
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[[Category: Rindgen D]]
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[[Category: Seganish, W M]]
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[[Category: Seganish WM]]
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[[Category: Tulshian, D]]
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[[Category: Tulshian D]]
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[[Category: Xiao, L]]
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[[Category: Van Rijn R]]
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[[Category: Zhang, X]]
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[[Category: Xiao L]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Zhang X]]
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[[Category: Mg binding]]
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[[Category: Zn binding]]
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Current revision

The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia

PDB ID 4dff

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