7ni4: Difference between revisions
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==Human ATM kinase domain with bound M4076 inhibitor== | ==Human ATM kinase domain with bound M4076 inhibitor== | ||
<StructureSection load='7ni4' size='340' side='right'caption='[[7ni4]]' scene=''> | <StructureSection load='7ni4' size='340' side='right'caption='[[7ni4]], [[Resolution|resolution]] 3.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7NI4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7NI4 FirstGlance]. <br> | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7NI4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7NI4 FirstGlance]. <br> | ||
</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=7ni4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7ni4 OCA], [https://pdbe.org/7ni4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7ni4 RCSB], [https://www.ebi.ac.uk/pdbsum/7ni4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7ni4 ProSAT]</span></td></tr> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=UGK:8-(1,3-dimethylpyrazol-4-yl)-1-(3-fluoranyl-5-methoxy-pyridin-4-yl)-7-methoxy-3-methyl-imidazo[4,5-c]quinolin-2-one'>UGK</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=7ni4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7ni4 OCA], [https://pdbe.org/7ni4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7ni4 RCSB], [https://www.ebi.ac.uk/pdbsum/7ni4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7ni4 ProSAT]</span></td></tr> | |||
</table> | </table> | ||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Human checkpoint kinase ataxia telangiectasia-mutated (ATM) plays a key role in initiation of the DNA damage response following DNA double-strand breaks. ATM inhibition is a promising approach in cancer therapy, but, so far, detailed insights into the binding modes of known ATM inhibitors have been hampered due to the lack of high-resolution ATM structures. Using cryo-EM, we have determined the structure of human ATM to an overall resolution sufficient to build a near-complete atomic model and identify two hitherto unknown zinc-binding motifs. We determined the structure of the kinase domain bound to ATPgammaS and to the ATM inhibitors KU-55933 and M4076 at 2.8 A, 2.8 A and 3.0 A resolution, respectively. The mode of action and selectivity of the ATM inhibitors can be explained by structural comparison and provide a framework for structure-based drug design. | |||
Molecular basis of human ATM kinase inhibition.,Stakyte K, Rotheneder M, Lammens K, Bartho JD, Gradler U, Fuchss T, Pehl U, Alt A, van de Logt E, Hopfner KP Nat Struct Mol Biol. 2021 Sep 23. pii: 10.1038/s41594-021-00654-x. doi:, 10.1038/s41594-021-00654-x. PMID:34556870<ref>PMID:34556870</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 7ni4" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Latest revision as of 08:56, 14 July 2024
Human ATM kinase domain with bound M4076 inhibitor
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