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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]] 1.90&Aring;' scene=''>
<StructureSection load='4ajf' size='340' side='right'caption='[[4ajf]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<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>
<table><tr><td colspan='2'>[[4ajf]] 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=4AJF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/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='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.9&#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]], [[4ajg|4ajg]], [[4ajm|4ajm]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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='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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4ajf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ajf OCA], [https://pdbe.org/4ajf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ajf RCSB], [https://www.ebi.ac.uk/pdbsum/4ajf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ajf 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/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Human]]
[[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 13:50, 9 May 2024

Identification and structural characterization of PDE10 fragment inhibitorsIdentification and structural characterization of PDE10 fragment inhibitors

Structural highlights

4ajf is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.9Å
Ligands:, ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

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 Also

References

  1. ↑ Wang H, Liu Y, Hou J, Zheng M, Robinson H, Ke H. Structural insight into substrate specificity of phosphodiesterase 10. Proc Natl Acad Sci U S A. 2007 Apr 3;104(14):5782-7. Epub 2007 Mar 26. PMID:17389385

4ajf, resolution 1.90Å

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