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3p1f

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{{STRUCTURE_3p1f| PDB=3p1f | SCENE= }}
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==Crystal structure of the bromodomain of human CREBBP in complex with a hydroquinazolin ligand==
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===Crystal structure of the bromodomain of human CREBBP in complex with a hydroquinazolin ligand===
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<StructureSection load='3p1f' size='340' side='right' caption='[[3p1f]], [[Resolution|resolution]] 1.63&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3p1f]] is a 2 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=3P1F OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3P1F FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3PF:3-METHYL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONE'>3PF</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3p1c|3p1c]], [[3p1d|3p1d]], [[3p1e|3p1e]]</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CREBBP ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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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<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=3p1f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3p1f OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3p1f RCSB], [http://www.ebi.ac.uk/pdbsum/3p1f 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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==Disease==
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==See Also==
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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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*[[CREB-binding protein|CREB-binding protein]]
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== References ==
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==Function==
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<references/>
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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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__TOC__
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</StructureSection>
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==About this Structure==
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[[3p1f]] is a 2 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=3P1F OCA].
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==Reference==
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<references group="xtra"/><references/>
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[[Category: Histone acetyltransferase]]
[[Category: Histone acetyltransferase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Arrowsmith, C H.]]
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[[Category: Arrowsmith, C H]]
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[[Category: Bountra, C.]]
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[[Category: Bountra, C]]
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[[Category: Delft, F Von.]]
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[[Category: Delft, F Von]]
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[[Category: Edwards, A M.]]
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[[Category: Edwards, A M]]
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[[Category: Fedorov, O.]]
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[[Category: Fedorov, O]]
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[[Category: Filippakopoulos, P.]]
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[[Category: Filippakopoulos, P]]
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[[Category: Knapp, S.]]
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[[Category: Knapp, S]]
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[[Category: Muniz, J.]]
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[[Category: Muniz, J]]
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[[Category: Picaud, S.]]
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[[Category: Picaud, S]]
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[[Category: SGC, Structural Genomics Consortium.]]
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[[Category: Structural genomic]]
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[[Category: Weigelt, J.]]
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[[Category: Weigelt, J]]
[[Category: Bromodomain]]
[[Category: Bromodomain]]
[[Category: Cbp]]
[[Category: Cbp]]
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[[Category: Crebbp]]
[[Category: Crebbp]]
[[Category: Kat3a]]
[[Category: Kat3a]]
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[[Category: Rst]]
 
[[Category: Rst]]
[[Category: Rst]]
[[Category: Sgc]]
[[Category: Sgc]]
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[[Category: Structural genomics consortium]]
 
[[Category: Transcription]]
[[Category: Transcription]]

Revision as of 07:22, 19 December 2014

Crystal structure of the bromodomain of human CREBBP in complex with a hydroquinazolin ligand

3p1f, resolution 1.63Å

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