3u4u
From Proteopedia
(Difference between revisions)
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<StructureSection load='3u4u' size='340' side='right' caption='[[3u4u]], [[Resolution|resolution]] 2.20Å' scene=''> | <StructureSection load='3u4u' size='340' side='right' caption='[[3u4u]], [[Resolution|resolution]] 2.20Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[3u4u]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/ | + | <table><tr><td colspan='2'>[[3u4u]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3U4U OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3U4U FirstGlance]. <br> |
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=LNH:3-{5-(ACETYLAMINO)-3-[3-CYANO-7-(CYCLOPROPYLAMINO)PYRAZOLO[1,5-A]PYRIMIDIN-5-YL]-1H-INDOL-1-YL}PROPANOIC+ACID'>LNH</scene><br> | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=LNH:3-{5-(ACETYLAMINO)-3-[3-CYANO-7-(CYCLOPROPYLAMINO)PYRAZOLO[1,5-A]PYRIMIDIN-5-YL]-1H-INDOL-1-YL}PROPANOIC+ACID'>LNH</scene><br> | ||
| - | <tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CSNK2A1, CK2A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 | + | <tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CSNK2A1, CK2A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> |
<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr> | <tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr> | ||
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3u4u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3u4u OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3u4u RCSB], [http://www.ebi.ac.uk/pdbsum/3u4u PDBsum]</span></td></tr> | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3u4u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3u4u OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3u4u RCSB], [http://www.ebi.ac.uk/pdbsum/3u4u PDBsum]</span></td></tr> | ||
<table> | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described. | ||
| + | |||
| + | Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.,Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. doi: 10.1021/ml200257n. eCollection, 2012 Apr 12. PMID:24900464<ref>PMID:24900464</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
==See Also== | ==See Also== | ||
*[[Casein kinase|Casein kinase]] | *[[Casein kinase|Casein kinase]] | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Human]] |
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Dowling, J.]] | [[Category: Dowling, J.]] | ||
Revision as of 06:18, 24 September 2014
Casein kinase 2 in complex with AZ-Inhibitor
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