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4jds

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{{STRUCTURE_4jds| PDB=4jds | SCENE= }}
 
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===SETD7 in complex with inhibitor PF-5426 and S-adenosyl-methionine===
 
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==Function==
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==SETD7 in complex with inhibitor PF-5426 and S-adenosyl-methionine==
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[[http://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>
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<StructureSection load='4jds' size='340' side='right'caption='[[4jds]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
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== Structural highlights ==
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<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>
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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]] 1.7&#8491;</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=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>
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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=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>
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</table>
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== Function ==
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[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>
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==About this Structure==
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==See Also==
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[[4jds]] is a 4 chain structure with sequence from [http://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].
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*[[Histone methyltransferase 3D structures|Histone methyltransferase 3D structures]]
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== References ==
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==Reference==
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<references/>
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<references group="xtra"/><references/>
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__TOC__
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[[Category: Histone-lysine N-methyltransferase]]
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Arrowsmith, C H.]]
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[[Category: Large Structures]]
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[[Category: Bakkouri, M El.]]
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[[Category: Arrowsmith CH]]
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[[Category: Barsyte, D.]]
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[[Category: Barsyte D]]
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[[Category: Bountra, C.]]
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[[Category: Bountra C]]
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[[Category: Brown, P J.]]
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[[Category: Brown PJ]]
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[[Category: Bunnage, M.]]
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[[Category: Bunnage M]]
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[[Category: Dong, A.]]
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[[Category: Dong A]]
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[[Category: Edwards, A M.]]
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[[Category: Edwards AM]]
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[[Category: Owen, D.]]
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[[Category: El Bakkouri M]]
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[[Category: Park, H.]]
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[[Category: Owen D]]
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[[Category: SGC, Structural Genomics Consortium.]]
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[[Category: Park H]]
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[[Category: Tatlock, J.]]
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[[Category: Tatlock J]]
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[[Category: Vedadi, M.]]
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[[Category: Vedadi M]]
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[[Category: Wu, H.]]
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[[Category: Wu H]]
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[[Category: Zeng, H.]]
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[[Category: Zeng H]]
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[[Category: Histone lysine methyltransferase]]
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[[Category: Histone modification]]
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[[Category: Inhibitor]]
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[[Category: Methyltransferase]]
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[[Category: Pf-5426]]
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[[Category: S-adenosyl-l-methionine]]
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[[Category: Sam]]
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[[Category: Set domain]]
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[[Category: Setd7]]
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[[Category: Sgc]]
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[[Category: Structural genomics consortium]]
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[[Category: Transcription regulation]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

SETD7 in complex with inhibitor PF-5426 and S-adenosyl-methionine

PDB ID 4jds

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