This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
3uuo
From Proteopedia
| Line 1: | Line 1: | ||
==The discovery of potent, selectivity, and orally bioavailable pyrozoloquinolines as PDE10 inhibitors for the treatment of Schizophrenia== | ==The discovery of potent, selectivity, and orally bioavailable pyrozoloquinolines as PDE10 inhibitors for the treatment of Schizophrenia== | ||
| - | <StructureSection load='3uuo' size='340' side='right' caption='[[3uuo]], [[Resolution|resolution]] 2.11Å' scene=''> | + | <StructureSection load='3uuo' size='340' side='right'caption='[[3uuo]], [[Resolution|resolution]] 2.11Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[3uuo]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[3uuo]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3UUO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3UUO FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0CV:6-METHOXY-3,8-DIMETHYL-4-(PIPERAZIN-1-YL)-1H-PYRAZOLO[3,4-B]QUINOLINE'>0CV</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</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" id="ligandDat"><scene name='pdbligand=0CV:6-METHOXY-3,8-DIMETHYL-4-(PIPERAZIN-1-YL)-1H-PYRAZOLO[3,4-B]QUINOLINE'>0CV</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PDE10A ([ | + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PDE10A ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3uuo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3uuo OCA], [https://pdbe.org/3uuo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3uuo RCSB], [https://www.ebi.ac.uk/pdbsum/3uuo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3uuo ProSAT]</span></td></tr> |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [[ | + | [[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 == | ||
| Line 21: | Line 21: | ||
==See Also== | ==See Also== | ||
| - | *[[Phosphodiesterase|Phosphodiesterase]] | + | *[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]] |
== References == | == References == | ||
<references/> | <references/> | ||
| Line 27: | Line 27: | ||
</StructureSection> | </StructureSection> | ||
[[Category: Human]] | [[Category: Human]] | ||
| + | [[Category: Large Structures]] | ||
[[Category: Bercovici, A]] | [[Category: Bercovici, A]] | ||
[[Category: Bleickardt, C]] | [[Category: Bleickardt, C]] | ||
Revision as of 08:08, 20 July 2022
The discovery of potent, selectivity, and orally bioavailable pyrozoloquinolines as PDE10 inhibitors for the treatment of Schizophrenia
| |||||||||||
Categories: Human | Large Structures | Bercovici, A | Bleickardt, C | Greenlee, W J | Guzzi, M | Ho, G D | Hodgson, R | Hruza, A | McElroy, W | Mckittrick, B | Mullins, D | Nechuta, T | Rindgen, D | Smith, E M | Smotryski, J | Tan, Z | Tulshian, D | Xiao, L | Yang, S | Zhang, X | Hydrolase | Hydrolase-hydrolase inhibitor complex | Inhibitor complex | Mg binding | Zn binding
