3s4q
From Proteopedia
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| - | [[ | + | ==P38 alpha kinase complexed with a pyrazolo-triazine based inhibitor== |
| + | <StructureSection load='3s4q' size='340' side='right' caption='[[3s4q]], [[Resolution|resolution]] 2.27Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3s4q]] 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=3S4Q OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3S4Q FirstGlance]. <br> | ||
| + | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=NK0:3-[(6-BENZOYL-5-METHYLPYRROLO[2,1-F][1,2,4]TRIAZIN-4-YL)AMINO]-N-CYCLOPROPYL-4-METHYLBENZAMIDE'>NK0</scene><br> | ||
| + | <tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CSBP, CSBP1, CSBP2, CSPB1, MAPK14, MXI2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr> | ||
| + | <tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] </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=3s4q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3s4q OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3s4q RCSB], [http://www.ebi.ac.uk/pdbsum/3s4q PDBsum]</span></td></tr> | ||
| + | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38alpha have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation. | ||
| - | + | Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38alpha MAP kinase inhibitors.,Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. Epub 2011 May 30. PMID:21705217<ref>PMID:21705217</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| - | + | ==See Also== | |
| - | + | *[[Mitogen-activated protein kinase|Mitogen-activated protein kinase]] | |
| - | == | + | == References == |
| - | [[ | + | <references/> |
| - | + | __TOC__ | |
| - | == | + | </StructureSection> |
| - | < | + | |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Mitogen-activated protein kinase]] | [[Category: Mitogen-activated protein kinase]] | ||
Revision as of 06:55, 9 June 2014
P38 alpha kinase complexed with a pyrazolo-triazine based inhibitor
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