5i89

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'''Unreleased structure'''
 
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The entry 5i89 is ON HOLD until Paper Publication
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==Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02857790==
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<StructureSection load='5i89' size='340' side='right' caption='[[5i89]], [[Resolution|resolution]] 1.07&Aring;' scene=''>
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Authors: Setser, J.W., Poy, F., Bellon, S.F.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5i89]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I89 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I89 FirstGlance]. <br>
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Description: Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02857790
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=69B:(4R)-6-(3-CYCLOPROPYL-1-METHYL-1H-INDAZOL-5-YL)-4-METHYL-1,3,4,5-TETRAHYDRO-2H-1,5-BENZODIAZEPIN-2-ONE'>69B</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene></td></tr>
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[[Category: Unreleased Structures]]
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5i83|5i83]], [[5i86|5i86]]</td></tr>
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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=5i89 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i89 OCA], [http://pdbe.org/5i89 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i89 RCSB], [http://www.ebi.ac.uk/pdbsum/5i89 PDBsum]</span></td></tr>
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</table>
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== Disease ==
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[[http://www.uniprot.org/uniprot/CBP_HUMAN CBP_HUMAN]] Note=Chromosomal aberrations involving CREBBP may be a cause of acute myeloid leukemias. Translocation t(8;16)(p11;p13) with KAT6A; translocation t(11;16)(q23;p13.3) with MLL/HRX; translocation t(10;16)(q22;p13) with KAT6B. KAT6A-CREBBP may induce leukemia by inhibiting RUNX1-mediated transcription. Defects in CREBBP are a cause of Rubinstein-Taybi syndrome type 1 (RSTS1) [MIM:[http://omim.org/entry/180849 180849]]. RSTS1 is an autosomal dominant disorder characterized by craniofacial abnormalities, broad thumbs, broad big toes, mental retardation and a propensity for development of malignancies.<ref>PMID:11331617</ref> <ref>PMID:12114483</ref> <ref>PMID:12566391</ref> <ref>PMID:15706485</ref>
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== Function ==
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[[http://www.uniprot.org/uniprot/CBP_HUMAN CBP_HUMAN]] Acetylates histones, giving a specific tag for transcriptional activation. Also acetylates non-histone proteins, like NCOA3 and FOXO1. Binds specifically to phosphorylated CREB and enhances its transcriptional activity toward cAMP-responsive genes. Acts as a coactivator of ALX1 in the presence of EP300.<ref>PMID:9707565</ref> <ref>PMID:11154691</ref> <ref>PMID:12738767</ref> <ref>PMID:12929931</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: Bellon, S F]]
[[Category: Poy, F]]
[[Category: Poy, F]]
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[[Category: Bellon, S.F]]
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[[Category: Setser, J W]]
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[[Category: Setser, J.W]]
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[[Category: Bromodomain inhibitor]]
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[[Category: Protein binding-inhibitor complex]]

Revision as of 18:49, 12 May 2016

Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02857790

5i89, resolution 1.07Å

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