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==Crystal Structure of Human DOT1L in Complex with a Selective Inhibitor==
==Crystal Structure of Human DOT1L in Complex with a Selective Inhibitor==
<StructureSection load='3sr4' size='340' side='right' caption='[[3sr4]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
<StructureSection load='3sr4' size='340' side='right'caption='[[3sr4]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[3sr4]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3SR4 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3SR4 FirstGlance]. <br>
<table><tr><td colspan='2'>[[3sr4]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3SR4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3SR4 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=TT8:(2S)-2-AZANYL-4-[[(2S,3S,4R,5R)-5-[6-(METHYLAMINO)PURIN-9-YL]-3,4-BIS(OXIDANYL)OXOLAN-2-YL]METHYLSULFANYL]BUTANOIC+ACID'>TT8</scene></td></tr>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=TT8:(2S)-2-AZANYL-4-[[(2S,3S,4R,5R)-5-[6-(METHYLAMINO)PURIN-9-YL]-3,4-BIS(OXIDANYL)OXOLAN-2-YL]METHYLSULFANYL]BUTANOIC+ACID'>TT8</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1nw3|1nw3]], [[3qow|3qow]], [[3qox|3qox]]</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1nw3|1nw3]], [[3qow|3qow]], [[3qox|3qox]]</div></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">DOT1L, KIAA1814, KMT4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">DOT1L, KIAA1814, KMT4 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone-lysine_N-methyltransferase Histone-lysine N-methyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.43 2.1.1.43] </span></td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Histone-lysine_N-methyltransferase Histone-lysine N-methyltransferase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.43 2.1.1.43] </span></td></tr>
<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=3sr4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3sr4 OCA], [http://pdbe.org/3sr4 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3sr4 RCSB], [http://www.ebi.ac.uk/pdbsum/3sr4 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3sr4 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=3sr4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3sr4 OCA], [https://pdbe.org/3sr4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3sr4 RCSB], [https://www.ebi.ac.uk/pdbsum/3sr4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3sr4 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/DOT1L_HUMAN DOT1L_HUMAN]] Histone methyltransferase. Methylates 'Lys-79' of histone H3. Nucleosomes are preferred as substrate compared to free histones. Binds to DNA.  
[[https://www.uniprot.org/uniprot/DOT1L_HUMAN DOT1L_HUMAN]] Histone methyltransferase. Methylates 'Lys-79' of histone H3. Nucleosomes are preferred as substrate compared to free histones. Binds to DNA.  
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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==See Also==
==See Also==
*[[Histone methyltransferase|Histone methyltransferase]]
*[[Histone methyltransferase 3D structures|Histone methyltransferase 3D structures]]
== References ==
== References ==
<references/>
<references/>
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[[Category: Histone-lysine N-methyltransferase]]
[[Category: Histone-lysine N-methyltransferase]]
[[Category: Human]]
[[Category: Human]]
[[Category: Large Structures]]
[[Category: Chen, P]]
[[Category: Chen, P]]
[[Category: Diao, J]]
[[Category: Diao, J]]

Revision as of 08:07, 29 June 2022

Crystal Structure of Human DOT1L in Complex with a Selective Inhibitor

3sr4, resolution 2.50Å

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