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5x73

From Proteopedia

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'''Unreleased structure'''
 
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The entry 5x73 is ON HOLD
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==The crystal Structure PDE delta in complex with R-p9==
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<StructureSection load='5x73' size='340' side='right'caption='[[5x73]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5x73]] is a 1 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=5X73 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5X73 FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.5&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=P59:(2R)-2-(2-fluorophenyl)-3-phenyl-1,2-dihydroquinazolin-4-one'>P59</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5x73 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5x73 OCA], [https://pdbe.org/5x73 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5x73 RCSB], [https://www.ebi.ac.uk/pdbsum/5x73 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5x73 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PDE6D_HUMAN PDE6D_HUMAN] Acts as a GTP specific dissociation inhibitor (GDI). Increases the affinity of ARL3 for GTP by several orders of magnitude and does so by decreasing the nucleotide dissociation rate. Stabilizes Arl3-GTP by decreasing the nucleotide dissociation (By similarity).
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Structural biology is a powerful tool for investigating the stereospecific interactions between a protein and its ligand. Herein, an unprecedented chiral binding pattern was observed for inhibitors of KRAS-PDEdelta interactions. Virtual screening and X-ray crystallography studies revealed that two enantiomers of a racemic inhibitor could bind at different sites. Fragment-based drug design was used to identify highly potent PDEdelta inhibitors that can be used as promising lead compounds for target validation and antitumor drug development.
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Authors:
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Structural Biology-Inspired Discovery of Novel KRAS-PDEdelta Inhibitors.,Jiang Y, Zhuang C, Chen L, Lu J, Dong G, Miao Z, Zhang W, Li J, Sheng C J Med Chem. 2017 Oct 3. doi: 10.1021/acs.jmedchem.7b01243. PMID:28929751<ref>PMID:28929751</ref>
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Description:
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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<div class="pdbe-citations 5x73" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Chen L]]
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[[Category: Jiang Y]]
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[[Category: Sheng C]]
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[[Category: Wang F]]
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[[Category: Wang R]]
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[[Category: Zhuang C]]

Current revision

The crystal Structure PDE delta in complex with R-p9

PDB ID 5x73

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