4jds: Difference between revisions
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==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=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[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]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/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='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">SETD7, KIAA1717, KMT7, SET7, SET9 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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='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=4jds FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4jds OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4jds RCSB], [http://www.ebi.ac.uk/pdbsum/4jds PDBsum]</span></td></tr> | |||
</table> | |||
== Function == | |||
[[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> | |||
== | ==See Also== | ||
[[ | *[[Histone methyltransferase|Histone methyltransferase]] | ||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
== | |||
<references | |||
[[Category: Histone-lysine N-methyltransferase]] | [[Category: Histone-lysine N-methyltransferase]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Arrowsmith, C H | [[Category: Arrowsmith, C H]] | ||
[[Category: Bakkouri, M El | [[Category: Bakkouri, M El]] | ||
[[Category: Barsyte, D | [[Category: Barsyte, D]] | ||
[[Category: Bountra, C | [[Category: Bountra, C]] | ||
[[Category: Brown, P J | [[Category: Brown, P J]] | ||
[[Category: Bunnage, M | [[Category: Bunnage, M]] | ||
[[Category: Dong, A | [[Category: Dong, A]] | ||
[[Category: Edwards, A M | [[Category: Edwards, A M]] | ||
[[Category: Owen, D | [[Category: Owen, D]] | ||
[[Category: Park, H | [[Category: Park, H]] | ||
[[Category: | [[Category: Structural genomic]] | ||
[[Category: Tatlock, J | [[Category: Tatlock, J]] | ||
[[Category: Vedadi, M | [[Category: Vedadi, M]] | ||
[[Category: Wu, H | [[Category: Wu, H]] | ||
[[Category: Zeng, H | [[Category: Zeng, H]] | ||
[[Category: Histone lysine methyltransferase]] | [[Category: Histone lysine methyltransferase]] | ||
[[Category: Histone modification]] | [[Category: Histone modification]] | ||
| Line 37: | Line 44: | ||
[[Category: Setd7]] | [[Category: Setd7]] | ||
[[Category: Sgc]] | [[Category: Sgc]] | ||
[[Category: Transcription regulation]] | [[Category: Transcription regulation]] | ||
[[Category: Transferase-transferase inhibitor complex]] | [[Category: Transferase-transferase inhibitor complex]] | ||
