3rgf
From Proteopedia
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| - | [[ | + | ==Crystal Structure of human CDK8/CycC== |
| + | <StructureSection load='3rgf' size='340' side='right' caption='[[3rgf]], [[Resolution|resolution]] 2.20Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3rgf]] is a 2 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=3RGF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RGF FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BAX:4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE'>BAX</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CDK8 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), CCNC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3rgf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rgf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rgf RCSB], [http://www.ebi.ac.uk/pdbsum/3rgf PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Cyclin-dependent kinase (CDK) 8 associates with cyclin C (CycC) and belongs to the CDK module of the Mediator of transcription, together with MED12 and MED13. CDK8 is involved in the regulation of mRNA transcription and was identified as a potent oncogene in colon cancerogenesis. We have solved the 2.2-A crystal structure of CDK8/CycC in complex with sorafenib, an anti-cancer drug of clinical relevance. The CDK8 structure reveals a unique CycC recognition helix that explains the specificity of the CDK8/CycC pair and discrimination among the highly promiscuous binding in the CDK/cyclin family. In contrast to all CDKs, the CDK8 activation loop appears not to be phosphorylated. Based on the structure, we discuss an alternate mode of CDK8 activation to the general CDK activation by T-loop phosphorylation. Sorafenib binds to the catalytic cleft of CDK8. It displays a deep pocket binding mode and is the first small molecule to induce a DFG-out conformation in the CDK family, which is actually DMG-out in CDK8. | ||
| - | + | The Structure of CDK8/CycC Implicates Specificity in the CDK/Cyclin Family and Reveals Interaction with a Deep Pocket Binder.,Schneider EV, Bottcher J, Blaesse M, Neumann L, Huber R, Maskos K J Mol Biol. 2011 Sep 16;412(2):251-66. Epub 2011 Jul 23. PMID:21806996<ref>PMID:21806996</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
| + | *[[Cyclin|Cyclin]] | ||
*[[Cyclin-dependent kinase|Cyclin-dependent kinase]] | *[[Cyclin-dependent kinase|Cyclin-dependent kinase]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: Blaesse, M | + | [[Category: Blaesse, M]] |
| - | [[Category: Boettcher, J | + | [[Category: Boettcher, J]] |
| - | [[Category: Huber, R | + | [[Category: Huber, R]] |
| - | [[Category: Maskos, K | + | [[Category: Maskos, K]] |
| - | [[Category: Schneider, E V | + | [[Category: Schneider, E V]] |
[[Category: Protein kinase complex]] | [[Category: Protein kinase complex]] | ||
[[Category: Transcription]] | [[Category: Transcription]] | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
Revision as of 12:43, 9 December 2014
Crystal Structure of human CDK8/CycC
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