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{{STRUCTURE_4nyv|  PDB=4nyv  |  SCENE=  }}
===Crystal Structure of the Bromodomain of human CREBBP in complex with a quinazolin-one ligand===


==Disease==
==Crystal Structure of the Bromodomain of human CREBBP in complex with a quinazolin-one ligand==
[[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>
<StructureSection load='4nyv' size='340' side='right'caption='[[4nyv]], [[Resolution|resolution]] 1.83&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4nyv]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NYV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4NYV FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.83&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=15E:6-BROMO-3-METHYL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONE'>15E</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4nyv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nyv OCA], [https://pdbe.org/4nyv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4nyv RCSB], [https://www.ebi.ac.uk/pdbsum/4nyv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4nyv ProSAT]</span></td></tr>
</table>
== Disease ==
[https://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:[https://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>  
== Function ==
[https://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>


==Function==
==See Also==
[[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> 
*[[CREB-binding protein 3D structures|CREB-binding protein 3D structures]]
 
== References ==
==About this Structure==
<references/>
[[4nyv]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NYV OCA].
__TOC__
 
</StructureSection>
==Reference==
[[Category: Homo sapiens]]
<references group="xtra"/><references/>
[[Category: Large Structures]]
[[Category: Arrowsmith, C H.]]
[[Category: Arrowsmith CH]]
[[Category: Bountra, C.]]
[[Category: Bountra C]]
[[Category: Brennan, P.]]
[[Category: Brennan P]]
[[Category: Delft, F Von.]]
[[Category: Edwards AM]]
[[Category: Edwards, A M.]]
[[Category: Fedorov O]]
[[Category: Fedorov, O.]]
[[Category: Felletar I]]
[[Category: Felletar, I.]]
[[Category: Filippakopoulos P]]
[[Category: Filippakopoulos, P.]]
[[Category: Knapp S]]
[[Category: Knapp, S.]]
[[Category: Martin S]]
[[Category: Martin, S.]]
[[Category: Monteiro OP]]
[[Category: Monteiro, O P.]]
[[Category: Picaud S]]
[[Category: Picaud, S.]]
[[Category: Von Delft F]]
[[Category: SGC, Structural Genomics Consortium.]]
[[Category: Bromodomain]]
[[Category: Creb binding]]
[[Category: Crebbp]]
[[Category: Kat3a]]
[[Category: Rst]]
[[Category: Rst]]
[[Category: Sgc]]
[[Category: Structural genomics consortium]]
[[Category: Transcription]]
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