3txo: Difference between revisions

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[[Image:3txo.jpg|left|200px]]


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==PKC eta kinase in complex with a naphthyridine==
The line below this paragraph, containing "STRUCTURE_3txo", creates the "Structure Box" on the page.
<StructureSection load='3txo' size='340' side='right'caption='[[3txo]], [[Resolution|resolution]] 2.05&Aring;' scene=''>
You may change the PDB parameter (which sets the PDB file loaded into the applet)  
== Structural highlights ==
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
<table><tr><td colspan='2'>[[3txo]] 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=3TXO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3TXO FirstGlance]. <br>
or leave the SCENE parameter empty for the default display.
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.05&#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=07U:2-METHYL-N~1~-[3-(PYRIDIN-4-YL)-2,6-NAPHTHYRIDIN-1-YL]PROPANE-1,2-DIAMINE'>07U</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
{{STRUCTURE_3txo|  PDB=3txo  |  SCENE=  }}
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3txo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3txo OCA], [https://pdbe.org/3txo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3txo RCSB], [https://www.ebi.ac.uk/pdbsum/3txo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3txo ProSAT]</span></td></tr>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The present study describes a novel series of ATP-competitive PKC inhibitors based on the 2,6-naphthyridine template. Example compounds potently inhibit the novel Protein Kinase C (PKC) isotypes delta, epsilon, eta, theta (in particular PKCepsilon/eta, and display a 10-100-fold selectivity over the classical PKC isotypes. The prototype compound 11 was found to inhibit PKCtheta-dependent pathways in vitro and in vivo. In vitro, a-CD3/a-CD28-induced lymphocyte proliferation could be effectively blocked in 10% rat whole blood. In mice, 11 dose-dependently inhibited Staphylococcus aureus enterotoxin B-triggered IL-2 serum levels after oral dosing.


===PKC eta kinase in complex with a naphthyridine===
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.,van Eis MJ, Evenou JP, Floersheim P, Gaul C, Cowan-Jacob SW, Monovich L, Rummel G, Schuler W, Stark W, Strauss A, Matt A, Vangrevelinghe E, Wagner J, Soldermann N Bioorg Med Chem Lett. 2011 Dec 15;21(24):7367-72. Epub 2011 Oct 21. PMID:22078216<ref>PMID:22078216</ref>


From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 3txo" style="background-color:#fffaf0;"></div>


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==See Also==
The line below this paragraph, {{ABSTRACT_PUBMED_22078216}}, adds the Publication Abstract to the page
*[[Protein kinase C 3D structures|Protein kinase C 3D structures]]
(as it appears on PubMed at http://www.pubmed.gov), where 22078216 is the PubMed ID number.
== References ==
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<references/>
{{ABSTRACT_PUBMED_22078216}}
__TOC__
 
</StructureSection>
==About this Structure==
[[3txo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TXO OCA].
 
==Reference==
<ref group="xtra">PMID:022078216</ref><references group="xtra"/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein kinase C]]
[[Category: Large Structures]]
[[Category: Cowan-Jacob, S W.]]
[[Category: Cowan-Jacob SW]]
[[Category: Rummel, G.]]
[[Category: Rummel G]]
[[Category: Stark, W.]]
[[Category: Stark W]]
[[Category: Kinase]]
[[Category: Phosphotransferase]]
[[Category: Transferase-transferase inhibitor complex]]

Latest revision as of 02:28, 21 November 2024

PKC eta kinase in complex with a naphthyridine

3txo, resolution 2.05Å

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