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[[Image:3tnw.png|left|200px]]
==Structure of CDK2/cyclin A in complex with CAN508==
<StructureSection load='3tnw' size='340' side='right' caption='[[3tnw]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[3tnw]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TNW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3TNW FirstGlance]. <br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=F18:4-[(E)-(3,5-DIAMINO-1H-PYRAZOL-4-YL)DIAZENYL]PHENOL'>F18</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene><br>
<tr><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), CCNA, CCNA2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus])</td></tr>
<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </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=3tnw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tnw OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3tnw RCSB], [http://www.ebi.ac.uk/pdbsum/3tnw PDBsum]</span></td></tr>
<table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
CDK9 is the kinase of positive transcription elongation factor b and facilitates the transition of paused RNA polymerase II to processive transcription elongation. CDK9 is a validated target for the treatment of cancer, cardiac hypertrophy, and human immunodeficiency virus. Here we analyze different CDK9/cyclin T variants to identify a form of the complex amenable to use in inhibitor design. To demonstrate the utility of this system, we have determined the crystal structures of CDK9/cyclin T and CDK2/cyclin A bound to the CDK9-specific inhibitor CAN508. Comparison of the structures reveals CDK9-specific conformational changes and identifies a CDK9-specific hydrophobic pocket, adjacent to the alphaC-helix. By comparison with a previously published structure of CDK9/cyclin T/human immunodeficiency virus TAT we find that the CDK9 alphaC-helix has a degree of conformational variability that has the potential to be exploited for inhibitor design.


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The CDK9 C-helix Exhibits Conformational Plasticity That May Explain the Selectivity of CAN508.,Baumli S, Hole AJ, Noble ME, Endicott JA ACS Chem Biol. 2012 Feb 10. PMID:22292676<ref>PMID:22292676</ref>
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{{STRUCTURE_3tnw|  PDB=3tnw  |  SCENE=  }}


===Structure of CDK2/cyclin A in complex with CAN508===
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
</div>


 
==See Also==
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*[[Cell division protein kinase|Cell division protein kinase]]
The line below this paragraph, {{ABSTRACT_PUBMED_22292676}}, adds the Publication Abstract to the page
*[[Cyclin|Cyclin]]
(as it appears on PubMed at http://www.pubmed.gov), where 22292676 is the PubMed ID number.
== References ==
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<references/>
{{ABSTRACT_PUBMED_22292676}}
__TOC__
 
</StructureSection>
==About this Structure==
[[3tnw]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TNW OCA].
 
==Reference==
<ref group="xtra">PMID:022292676</ref><references group="xtra"/>
[[Category: Bos taurus]]
[[Category: Bos taurus]]
[[Category: Cyclin-dependent kinase]]
[[Category: Cyclin-dependent kinase]]

Revision as of 06:01, 5 June 2014

Structure of CDK2/cyclin A in complex with CAN508

3tnw, resolution 2.00Å

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