7ukz
From Proteopedia
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<table><tr><td colspan='2'>[[7ukz]] is a 6 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=7UKZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7UKZ FirstGlance]. <br> | <table><tr><td colspan='2'>[[7ukz]] is a 6 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=7UKZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7UKZ FirstGlance]. <br> | ||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.6Å</td></tr> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.6Å</td></tr> | ||
| - | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NK3: | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NK3:9-[4-[(2~{R})-1-(dimethylamino)propan-2-yl]phenyl]-6-methyl-8-oxidanyl-5~{H}-thieno[2,3-c]quinolin-4-one'>NK3</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr> |
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7ukz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7ukz OCA], [https://pdbe.org/7ukz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7ukz RCSB], [https://www.ebi.ac.uk/pdbsum/7ukz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7ukz ProSAT]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7ukz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7ukz OCA], [https://pdbe.org/7ukz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7ukz RCSB], [https://www.ebi.ac.uk/pdbsum/7ukz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7ukz ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| - | == | + | <div style="background-color:#fffaf0;"> |
| - | + | == Publication Abstract from PubMed == | |
| + | CDK11 is a cyclin-dependent kinase that controls proliferation by regulating transcription, RNA splicing, and the cell cycle. As its activity is increasingly associated with cancer, CDK11 is an attractive target for the development of small-molecule inhibitors. However, the development of CDK11 inhibitors with limited off-target effects against other CDKs poses a challenge based on the high conservation of sequence across family members. OTS964 is notable as it displays a measure of specificity for CDK11 in cells. To understand the basis for OTS964's specificity for CDK11, we solved a 2.6 A crystal structure of the CDK11 kinase domain bound to OTS964. Despite the absence of cyclin, CDK11 adopts an active-like conformation when bound to OTS964. We identified amino acids likely to contribute to the specificity of OTS964 for CDK11 and assessed their contribution to OTS964 binding by isothermal titration calorimetry (ITC) in vitro and by resistance to OTS964 in cells. | ||
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| + | Crystal structure of the CDK11 kinase domain bound to the small-molecule inhibitor OTS964.,Kelso S, O'Brien S, Kurinov I, Angers S, Sicheri F Structure. 2022 Dec 1;30(12):1615-1625.e4. doi: 10.1016/j.str.2022.10.003. Epub , 2022 Nov 2. PMID:36327972<ref>PMID:36327972</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 7ukz" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
Current revision
CDK11 in complex with small molecule inhibitor OTS964
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