5ke2

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'''Unreleased structure'''
 
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The entry 5ke2 is ON HOLD
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==Crystal structure of SETDB1 Tudor domain in complex with inhibitor XST06472A==
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<StructureSection load='5ke2' size='340' side='right' caption='[[5ke2]], [[Resolution|resolution]] 1.56&Aring;' scene=''>
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Authors: Dong, A., Iqbal, A., Mader, P., Dobrovetsky, E., Twalker, J.R., Bountra, C., Arrowsmith, C.H., Edwards, A.M., Brown, P.J., Structural Genomics Consortium (SGC)
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5ke2]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KE2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5KE2 FirstGlance]. <br>
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Description: Crystal structure of SETDB1 Tudor domain in complex with fragment MRT0181a
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6S4:(3~{S})-~{N}-~{TERT}-BUTYL-1,2,3,4-TETRAHYDROISOQUINOLINE-3-CARBOXAMIDE'>6S4</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></td></tr>
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[[Category: Unreleased Structures]]
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<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=5ke2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ke2 OCA], [http://pdbe.org/5ke2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ke2 RCSB], [http://www.ebi.ac.uk/pdbsum/5ke2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ke2 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/SETB1_HUMAN SETB1_HUMAN]] Histone methyltransferase that specifically trimethylates 'Lys-9' of histone H3. H3 'Lys-9' trimethylation represents a specific tag for epigenetic transcriptional repression by recruiting HP1 (CBX1, CBX3 and/or CBX5) proteins to methylated histones. Mainly functions in euchromatin regions, thereby playing a central role in the silencing of euchromatic genes. H3 'Lys-9' trimethylation is coordinated with DNA methylation. Probably forms a complex with MBD1 and ATF7IP that represses transcription and couples DNA methylation and histone 'Lys-9' trimethylation. Its activity is dependent on MBD1 and is heritably maintained through DNA replication by being recruited by CAF-1. SETDB1 is targeted to histone H3 by TRIM28/TIF1B, a factor recruited by KRAB zinc-finger proteins.<ref>PMID:12869583</ref> <ref>PMID:14536086</ref> <ref>PMID:15327775</ref> <ref>PMID:17952062</ref>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Arrowsmith, C H]]
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[[Category: Bountra, C]]
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[[Category: Brown, P J]]
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[[Category: Dobrovetsky, E]]
[[Category: Dong, A]]
[[Category: Dong, A]]
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[[Category: Dobrovetsky, E]]
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[[Category: Edwards, A M]]
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[[Category: Twalker, J.R]]
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[[Category: Iqbal, A]]
[[Category: Mader, P]]
[[Category: Mader, P]]
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[[Category: Bountra, C]]
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[[Category: Structural genomic]]
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[[Category: Arrowsmith, C.H]]
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[[Category: Walker, J R]]
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[[Category: Iqbal, A]]
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[[Category: Setdb1]]
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[[Category: Brown, P.J]]
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[[Category: Sgc]]
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[[Category: Edwards, A.M]]
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[[Category: Transcription]]
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[[Category: Structural Genomics Consortium (Sgc)]]
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[[Category: Tudor domain]]

Revision as of 11:50, 14 July 2016

Crystal structure of SETDB1 Tudor domain in complex with inhibitor XST06472A

5ke2, resolution 1.56Å

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