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4jds
From Proteopedia
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==SETD7 in complex with inhibitor PF-5426 and S-adenosyl-methionine== | ==SETD7 in complex with inhibitor PF-5426 and S-adenosyl-methionine== | ||
| - | <StructureSection load='4jds' size='340' side='right' caption='[[4jds]], [[Resolution|resolution]] 1.70Å' scene=''> | + | <StructureSection load='4jds' size='340' side='right'caption='[[4jds]], [[Resolution|resolution]] 1.70Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4jds]] is a 4 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[4jds]] 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=4JDS OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4JDS FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1L4:N-[(2R)-3-(3-CYANOPHENYL)-1-OXO-1-(PYRROLIDIN-1-YL)PROPAN-2-YL]-8-FLUORO-1,2,3,4-TETRAHYDROISOQUINOLINE-6-SULFONAMIDE'>1L4</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.7Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1L4:N-[(2R)-3-(3-CYANOPHENYL)-1-OXO-1-(PYRROLIDIN-1-YL)PROPAN-2-YL]-8-FLUORO-1,2,3,4-TETRAHYDROISOQUINOLINE-6-SULFONAMIDE'>1L4</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4jds FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4jds OCA], [https://pdbe.org/4jds PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4jds RCSB], [https://www.ebi.ac.uk/pdbsum/4jds PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4jds 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== | ==See Also== | ||
| - | *[[Histone methyltransferase|Histone methyltransferase]] | + | *[[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 D]] | |
| - | [[Category: Barsyte | + | [[Category: Bountra C]] |
| - | [[Category: Bountra | + | [[Category: Brown PJ]] |
| - | [[Category: Brown | + | [[Category: Bunnage M]] |
| - | [[Category: Bunnage | + | [[Category: Dong A]] |
| - | [[Category: Dong | + | [[Category: Edwards AM]] |
| - | [[Category: Edwards | + | [[Category: El Bakkouri M]] |
| - | [[Category: | + | [[Category: Owen D]] |
| - | [[Category: | + | [[Category: Park H]] |
| - | [[Category: | + | [[Category: Tatlock J]] |
| - | [[Category: Tatlock | + | [[Category: Vedadi M]] |
| - | [[Category: Vedadi | + | [[Category: Wu H]] |
| - | [[Category: Wu | + | [[Category: Zeng H]] |
| - | [[Category: Zeng | + | |
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Current revision
SETD7 in complex with inhibitor PF-5426 and S-adenosyl-methionine
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Categories: Homo sapiens | Large Structures | Arrowsmith CH | Barsyte D | Bountra C | Brown PJ | Bunnage M | Dong A | Edwards AM | El Bakkouri M | Owen D | Park H | Tatlock J | Vedadi M | Wu H | Zeng H
