5k9r
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==PDE10a with imidazopyrazine inhibitor== | |
| + | <StructureSection load='5k9r' size='340' side='right'caption='[[5k9r]], [[Resolution|resolution]] 2.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5k9r]] 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=5K9R OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5K9R FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6RC:4-[5-[1-(2-METHOXYETHYL)PYRAZOL-4-YL]-2-(QUINOLIN-2-YLOXYMETHYL)IMIDAZO[1,2-A]PYRAZIN-8-YL]MORPHOLINE'>6RC</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'>[https://proteopedia.org/fgij/fg.htm?mol=5k9r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5k9r OCA], [https://pdbe.org/5k9r PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5k9r RCSB], [https://www.ebi.ac.uk/pdbsum/5k9r PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5k9r ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == 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;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Design and optimization of a novel series of imidazo[1,2-b]pyridazine PDE10a inhibitors are described. Compound 31 displays excellent pharmacokinetic properties and was also evaluated as an insulin secretagogue in vitro and in vivo. | ||
| - | + | Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.,Meegalla SK, Huang H, Illig CR, Parks DJ, Chen J, Lee YK, Wilson KJ, Patel SK, Cheung WS, Lu T, Kirchner T, Askari HB, Geisler J, Patch RJ, Gibbs AC, Rady B, Connelly M, Player MR Bioorg Med Chem Lett. 2016 Sep 1;26(17):4216-22. doi: 10.1016/j.bmcl.2016.07.054., Epub 2016 Jul 25. PMID:27491708<ref>PMID:27491708</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 5k9r" style="background-color:#fffaf0;"></div> |
| - | [[Category: Gibbs | + | |
| + | ==See Also== | ||
| + | *[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Gibbs AG]] | ||
| + | [[Category: Schubert C]] | ||
Current revision
PDE10a with imidazopyrazine inhibitor
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