5u7r: Difference between revisions

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'''Unreleased structure'''


The entry 5u7r is ON HOLD
==Identification of A New Class of Potent Cdc7 Inhibitors Designed by Putative Pharmacophore Model: Synthesis and Biological Evaluation of 2,3-Dihydrothieno[3,2-d]pyrimidin-4(1H)-ones==
 
<StructureSection load='5u7r' size='340' side='right'caption='[[5u7r]], [[Resolution|resolution]] 3.33&Aring;' scene=''>
Authors: Hoffman, I.D., Skene, R.J.
== Structural highlights ==
 
<table><tr><td colspan='2'>[[5u7r]] is a 4 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=5U7R OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5U7R FirstGlance]. <br>
Description: Identification of A New Class of Potent Cdc7 Inhibitors Designed by Putative Pharmacophore Model: Synthesis and Biological Evaluation of 2,3-Dihydrothieno[3,2-d]pyrimidin-4(1H)-ones
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.33&#8491;</td></tr>
[[Category: Unreleased Structures]]
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=81G:(1S,4S)-4-(4-FLUOROPHENYL)-4-HYDROXY-6-(5-METHYL-1H-PYRAZOL-4-YL)-1H-SPIRO[CYCLOHEXANE-1,2-THIENO[3,2-D]PYRIMIDIN]-4(3H)-ONE'>81G</scene></td></tr>
[[Category: Hoffman, I.D]]
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5u7r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u7r OCA], [https://pdbe.org/5u7r PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5u7r RCSB], [https://www.ebi.ac.uk/pdbsum/5u7r PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5u7r ProSAT]</span></td></tr>
[[Category: Skene, R.J]]
</table>
== Function ==
[https://www.uniprot.org/uniprot/ROCK2_HUMAN ROCK2_HUMAN] Protein kinase which is a key regulator of actin cytoskeleton and cell polarity. Involved in regulation of smooth muscle contraction, actin cytoskeleton organization, stress fiber and focal adhesion formation, neurite retraction, cell adhesion and motility via phosphorylation of ADD1, BRCA2, CNN1, EZR, DPYSL2, EP300, MSN, MYL9/MLC2, NPM1, RDX, PPP1R12A and VIM. Phosphorylates SORL1 and IRF4. Acts as a negative regulator of VEGF-induced angiogenic endothelial cell activation. Positively regulates the activation of p42/MAPK1-p44/MAPK3 and of p90RSK/RPS6KA1 during myogenic differentiation. Plays an important role in the timely initiation of centrosome duplication. Inhibits keratinocyte terminal differentiation. May regulate closure of the eyelids and ventral body wall through organization of actomyosin bundles. Plays a critical role in the regulation of spine and synaptic properties in the hippocampus.<ref>PMID:10579722</ref> <ref>PMID:15699075</ref> <ref>PMID:16574662</ref> <ref>PMID:17015463</ref> <ref>PMID:19131646</ref> <ref>PMID:19997641</ref> <ref>PMID:21084279</ref> <ref>PMID:21147781</ref>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Hoffman ID]]
[[Category: Skene RJ]]

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