6oir

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<StructureSection load='6oir' size='340' side='right'caption='[[6oir]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
<StructureSection load='6oir' size='340' side='right'caption='[[6oir]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6oir]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6OIR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6OIR FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6oir]] is a 1 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=6OIR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6OIR FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MNJ:4-fluoro-N-(phenylsulfonyl)[1,1-biphenyl]-3-carbohydrazide'>MNJ</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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]] 2.03&#8491;</td></tr>
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<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ALY:N(6)-ACETYLLYSINE'>ALY</scene></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=ALY:N(6)-ACETYLLYSINE'>ALY</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MNJ:2-fluoranyl-5-phenyl-~{N}-(phenylsulfonyl)benzohydrazide'>MNJ</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </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=6oir FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6oir OCA], [https://pdbe.org/6oir PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6oir RCSB], [https://www.ebi.ac.uk/pdbsum/6oir PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6oir ProSAT]</span></td></tr>
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<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=6oir FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6oir OCA], [http://pdbe.org/6oir PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6oir RCSB], [http://www.ebi.ac.uk/pdbsum/6oir PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6oir ProSAT]</span></td></tr>
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</table>
</table>
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== Function ==
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<div style="background-color:#fffaf0;">
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[[http://www.uniprot.org/uniprot/KAT8_HUMAN KAT8_HUMAN]] Histone acetyltransferase which may be involved in transcriptional activation. May influence the function of ATM. As part of the MSL complex it is involved in acetylation of nucleosomal histone H4 producing specifically H4K16ac. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. That activity is less specific than the one of the MSL complex.<ref>PMID:12397079</ref> <ref>PMID:15923642</ref> <ref>PMID:20018852</ref>
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== Publication Abstract from PubMed ==
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A high-throughput screen for inhibitors of the histone acetyltransferase, KAT6A, led to identification of an aryl sulfonohydrazide derivative that inhibited KAT6A with an IC50 of 0.87M. Elaboration of the structure-activity relationship (SAR) and medicinal chemistry optimization led to discovery of WM-8014 (84), a highly potent inhibitor of KAT6A (IC50 = 0.008 M). WM-8014 competes with Ac-CoA and X-ray crystallographic analysis demonstrated binding to the Ac-CoA binding site. Through inhibition of KAT6A activity, WM-8014 induces cellular senescence and represents a unique pharmacological tool.
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Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A.,Leaver D, Cleary B, Nguyen NT, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White K, Katneni K, Cuellar M, Strasser J, Dahlin J, Walters MA, Street I, Monahan B, Jarman KE, Jousset Sabroux H, Falk H, Chung M, Hermans S, Parker MW, Thomas T, Baell JB J Med Chem. 2019 Jun 29. doi: 10.1021/acs.jmedchem.9b00665. PMID:31256587<ref>PMID:31256587</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 6oir" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Histone acetyltransferase 3D structures|Histone acetyltransferase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Histone acetyltransferase]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Baell, J B]]
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[[Category: Baell JB]]
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[[Category: Chung, M C]]
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[[Category: Chung MC]]
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[[Category: Hermans, S J]]
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[[Category: Hermans SJ]]
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[[Category: Parker, M W]]
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[[Category: Parker MW]]
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[[Category: Thomas, T]]
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[[Category: Thomas T]]
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[[Category: Complex]]
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[[Category: Inhibitor]]
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[[Category: Myst]]
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[[Category: Transferase]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

Crystal structure of MYST acetyltransferase domain in complex with inhibitor 62

PDB ID 6oir

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Proteopedia Page Contributors and Editors (what is this?)

OCA

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