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4anm

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Current revision (07:16, 1 May 2024) (edit) (undo)
 
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<StructureSection load='4anm' size='340' side='right'caption='[[4anm]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
<StructureSection load='4anm' size='340' side='right'caption='[[4anm]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4anm]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Maize Maize]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ANM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ANM FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4anm]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Zea_mays Zea mays]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ANM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ANM FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=WUL:8-BROMANYL-2-[[(3S)-3-OXIDANYLPYRROLIDIN-1-YL]METHYL]-3H-[1]BENZOFURO[3,2-D]PYRIMIDIN-4-ONE'>WUL</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.7&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1daw|1daw]], [[1day|1day]], [[1ds5|1ds5]], [[1f0q|1f0q]], [[1j91|1j91]], [[1jam|1jam]], [[1lp4|1lp4]], [[1lpu|1lpu]], [[1lr4|1lr4]], [[1m2p|1m2p]], [[1m2q|1m2q]], [[1m2r|1m2r]], [[1om1|1om1]], [[1zoe|1zoe]], [[1zog|1zog]], [[1zoh|1zoh]]</div></td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=WUL:8-BROMANYL-2-[[(3S)-3-OXIDANYLPYRROLIDIN-1-YL]METHYL]-3H-[1]BENZOFURO[3,2-D]PYRIMIDIN-4-ONE'>WUL</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4anm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4anm OCA], [https://pdbe.org/4anm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4anm RCSB], [https://www.ebi.ac.uk/pdbsum/4anm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4anm 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=4anm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4anm OCA], [https://pdbe.org/4anm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4anm RCSB], [https://www.ebi.ac.uk/pdbsum/4anm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4anm ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/CSK2A_MAIZE CSK2A_MAIZE]] Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. The alpha chain contains the catalytic site.
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[https://www.uniprot.org/uniprot/CSK2A_MAIZE CSK2A_MAIZE] Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. The alpha chain contains the catalytic site.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model.
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Discovery of XL413, a potent and selective CDC7 inhibitor.,Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M, Galan A, Holst CR, Huang P, Kane B, Kim MH, Li J, Markby D, Mohan M, Noson K, Plonowski A, Richards SJ, Robertson S, Shaw K, Stott G, Stout TJ, Young J, Yu P, Zaharia CA, Zhang W, Zhou P, Nuss JM, Xu W, Kearney PC Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. Epub 2012 Apr 16. PMID:22560567<ref>PMID:22560567</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4anm" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
*[[Casein kinase 3D structures|Casein kinase 3D structures]]
*[[Casein kinase 3D structures|Casein kinase 3D structures]]
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== References ==
 
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<references/>
 
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Maize]]
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[[Category: Zea mays]]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Stout TJ]]
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[[Category: Stout, T J]]
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[[Category: Transferase]]
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Current revision

Complex of CK2 with a CDC7 inhibitor

PDB ID 4anm

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