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==Development of a plate-based optical biosensor methodology to identify PDE10 fragment inhibitors==
==Development of a plate-based optical biosensor methodology to identify PDE10 fragment inhibitors==
<StructureSection load='4ajm' size='340' side='right' caption='[[4ajm]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
<StructureSection load='4ajm' size='340' side='right'caption='[[4ajm]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4ajm]] 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=4AJM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AJM FirstGlance]. <br>
<table><tr><td colspan='2'>[[4ajm]] 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=4AJM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4AJM FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3A6:3-AMINO-6-FLUORO-2-[4-(2-METHYLPYRIDIN-4-YL)PHENYL]-N-(METHYLSULFONYL)QUINOLINE-4-CARBOXAMIDE'>3A6</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4&#8491;</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]], [[4ajf|4ajf]], [[4ajg|4ajg]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3A6:3-AMINO-6-FLUORO-2-[4-(2-METHYLPYRIDIN-4-YL)PHENYL]-N-(METHYLSULFONYL)QUINOLINE-4-CARBOXAMIDE'>3A6</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></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=4ajm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ajm OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ajm RCSB], [http://www.ebi.ac.uk/pdbsum/4ajm PDBsum]</span></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=4ajm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ajm OCA], [https://pdbe.org/4ajm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ajm RCSB], [https://www.ebi.ac.uk/pdbsum/4ajm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ajm ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[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>
[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>  


==See Also==
==See Also==
*[[Phosphodiesterase|Phosphodiesterase]]
*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Aharony, D]]
[[Category: Large Structures]]
[[Category: Akerud, T]]
[[Category: Aharony D]]
[[Category: Albert, J S]]
[[Category: Akerud T]]
[[Category: Back, E]]
[[Category: Albert JS]]
[[Category: Geschwindner, S]]
[[Category: Back E]]
[[Category: Hillertz, P]]
[[Category: Geschwindner S]]
[[Category: Horsefeld, R]]
[[Category: Hillertz P]]
[[Category: Johansson, P]]
[[Category: Horsefeld R]]
[[Category: Scott, C]]
[[Category: Johansson P]]
[[Category: Spadola, L]]
[[Category: Scott C]]
[[Category: Spear, N]]
[[Category: Spadola L]]
[[Category: Tian, G]]
[[Category: Spear N]]
[[Category: Tigerstrom, A]]
[[Category: Tian G]]
[[Category: Hydrolase]]
[[Category: Tigerstrom A]]

Latest revision as of 10:50, 9 May 2024

Development of a plate-based optical biosensor methodology to identify PDE10 fragment inhibitors

4ajm, resolution 2.40Å

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