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==Identification and structural characterization of PDE10 fragment inhibitors== | ==Identification and structural characterization of PDE10 fragment inhibitors== | ||
<StructureSection load='4ajf' size='340' side='right' caption='[[4ajf]], [[Resolution|resolution]] 1.90Å' scene=''> | <StructureSection load='4ajf' size='340' side='right' caption='[[4ajf]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4ajf]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/ | <table><tr><td colspan='2'>[[4ajf]] is a 2 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=4AJF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AJF FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=F03:N-(4-OXO-3H-QUINAZOLIN-2-YL)ACETAMIDE'>F03</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=F03:N-(4-OXO-3H-QUINAZOLIN-2-YL)ACETAMIDE'>F03</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1lrb|1lrb]], [[2wey|2wey]], [[2y0j|2y0j]], [[4ael|4ael]], [[4ajd|4ajd]], [[4ajg|4ajg]], [[4ajm|4ajm]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1lrb|1lrb]], [[2wey|2wey]], [[2y0j|2y0j]], [[4ael|4ael]], [[4ajd|4ajd]], [[4ajg|4ajg]], [[4ajm|4ajm]]</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=4ajf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ajf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ajf RCSB], [http://www.ebi.ac.uk/pdbsum/4ajf PDBsum]</span></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=4ajf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ajf OCA], [http://pdbe.org/4ajf PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ajf RCSB], [http://www.ebi.ac.uk/pdbsum/4ajf PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ajf ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Human]] | ||
[[Category: Aharony, D]] | [[Category: Aharony, D]] | ||
[[Category: Akerud, T]] | [[Category: Akerud, T]] |
Revision as of 10:46, 4 August 2016
Identification and structural characterization of PDE10 fragment inhibitorsIdentification and structural characterization of PDE10 fragment inhibitors
Structural highlights
Function[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.[1] See AlsoReferences |
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