4e47: Difference between revisions
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==SET7/9 in complex with inhibitor (R)-(3-(3-cyanophenyl)-1-oxo-1-(pyrrolidin-1-yl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6- sulfonamide and S-adenosylmethionine== | ==SET7/9 in complex with inhibitor (R)-(3-(3-cyanophenyl)-1-oxo-1-(pyrrolidin-1-yl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6- sulfonamide and S-adenosylmethionine== | ||
<StructureSection load='4e47' size='340' side='right' caption='[[4e47]], [[Resolution|resolution]] 2.00Å' scene=''> | <StructureSection load='4e47' size='340' side='right'caption='[[4e47]], [[Resolution|resolution]] 2.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4e47]] is a 4 chain structure with sequence from [ | <table><tr><td colspan='2'>[[4e47]] is a 4 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=4E47 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4E47 FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0N6:(R)-(3-(3-CYANOPHENYL)-1-OXO-1-(PYRROLIDIN-1-YL)PROPAN-2-YL)-1,2,3,4-TETRAHYDROISOQUINOLINE-6-SULFONAMIDE'>0N6</scene>, <scene name='pdbligand=BME:BETA-MERCAPTOETHANOL'>BME</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0N6:(R)-(3-(3-CYANOPHENYL)-1-OXO-1-(PYRROLIDIN-1-YL)PROPAN-2-YL)-1,2,3,4-TETRAHYDROISOQUINOLINE-6-SULFONAMIDE'>0N6</scene>, <scene name='pdbligand=BME:BETA-MERCAPTOETHANOL'>BME</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=4e47 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4e47 OCA], [https://pdbe.org/4e47 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4e47 RCSB], [https://www.ebi.ac.uk/pdbsum/4e47 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4e47 ProSAT]</span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</table> | </table> | ||
== Function == | == Function == | ||
[[ | [[https://www.uniprot.org/uniprot/SETD7_HUMAN SETD7_HUMAN]] Histone methyltransferase that specifically monomethylates 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. Plays a central role in the transcriptional activation of genes such as collagenase or insulin. Recruited by IPF1/PDX-1 to the insulin promoter, leading to activate transcription. Has also methyltransferase activity toward non-histone proteins such as p53/TP53, TAF10, and possibly TAF7 by recognizing and binding the [KR]-[STA]-K in substrate proteins. Monomethylates 'Lys-189' of TAF10, leading to increase the affinity of TAF10 for RNA polymerase II. Monomethylates 'Lys-372' of p53/TP53, stabilizing p53/TP53 and increasing p53/TP53-mediated transcriptional activation.<ref>PMID:12588998</ref> <ref>PMID:15099517</ref> <ref>PMID:16141209</ref> <ref>PMID:17108971</ref> <ref>PMID:12540855</ref> <ref>PMID:15525938</ref> | ||
==See Also== | |||
*[[Histone methyltransferase 3D structures|Histone methyltransferase 3D structures]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: Arrowsmith | [[Category: Arrowsmith CH]] | ||
[[Category: Barsyte | [[Category: Barsyte D]] | ||
[[Category: Bountra | [[Category: Bountra C]] | ||
[[Category: Brown | [[Category: Brown PJ]] | ||
[[Category: Bunnage | [[Category: Bunnage M]] | ||
[[Category: Cook | [[Category: Cook A]] | ||
[[Category: Dong | [[Category: Dong A]] | ||
[[Category: Edwards | [[Category: Edwards AM]] | ||
[[Category: Fish | [[Category: Fish P]] | ||
[[Category: Ouyang | [[Category: Ouyang H]] | ||
[[Category: Owen | [[Category: Owen D]] | ||
[[Category: Tatlock J]] | |||
[[Category: Tatlock | [[Category: Vedadi M]] | ||
[[Category: Vedadi | [[Category: Walker JR]] | ||
[[Category: Walker | [[Category: Weigelt J]] | ||
[[Category: Weigelt | |||