4ts8

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'''Unreleased structure'''
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==Crystal structure of the bromodomain of human CREBBP in complex with XZ08==
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<StructureSection load='4ts8' size='340' side='right' caption='[[4ts8]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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The entry 4ts8 is ON HOLD until Paper Publication
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4ts8]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TS8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TS8 FirstGlance]. <br>
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Authors: Dong, J., Gartenmann, L., Spiliotopoulos, D., Caflisch, A.
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=XZ8:4-(1-ACETYL-1H-INDOL-3-YL)-5-METHYL-1,2-DIHYDRO-3H-PYRAZOL-3-ONE'>XZ8</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>
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Description: Crystal structure of the bromodomain of human CREBBP in complex with XZ08
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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=4ts8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ts8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ts8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ts8 PDBsum]</span></td></tr>
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[[Category: Unreleased Structures]]
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</table>
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[[Category: Dong, J]]
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== Disease ==
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[[Category: Spiliotopoulos, D]]
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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: Histone acetyltransferase]]
[[Category: Caflisch, A]]
[[Category: Caflisch, A]]
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[[Category: Dong, J]]
[[Category: Gartenmann, L]]
[[Category: Gartenmann, L]]
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[[Category: Spiliotopoulos, D]]
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[[Category: Inhibitor]]
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[[Category: Transcription]]
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[[Category: Transferase]]

Revision as of 12:20, 1 July 2015

Crystal structure of the bromodomain of human CREBBP in complex with XZ08

4ts8, resolution 2.00Å

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