4nyv

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{{STRUCTURE_4nyv| PDB=4nyv | SCENE= }}
 
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===Crystal Structure of the Bromodomain of human CREBBP in complex with a quinazolin-one ligand===
 
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==Disease==
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==Crystal Structure of the Bromodomain of human CREBBP in complex with a quinazolin-one ligand==
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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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<StructureSection load='4nyv' size='340' side='right'caption='[[4nyv]], [[Resolution|resolution]] 1.83&Aring;' scene=''>
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== Structural highlights ==
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<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>
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</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>
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<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>
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<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>
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</table>
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== Disease ==
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[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>
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== Function ==
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[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>
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==Function==
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==See Also==
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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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*[[CREB-binding protein 3D structures|CREB-binding protein 3D structures]]
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== References ==
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==About this Structure==
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<references/>
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[[4nyv]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NYV OCA].
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__TOC__
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</StructureSection>
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==Reference==
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[[Category: Homo sapiens]]
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<references group="xtra"/><references/>
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[[Category: Large Structures]]
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[[Category: Arrowsmith, C H.]]
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[[Category: Arrowsmith CH]]
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[[Category: Bountra, C.]]
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[[Category: Bountra C]]
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[[Category: Brennan, P.]]
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[[Category: Brennan P]]
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[[Category: Delft, F Von.]]
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[[Category: Edwards AM]]
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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: Felletar I]]
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[[Category: Felletar, I.]]
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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: Martin S]]
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[[Category: Martin, S.]]
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[[Category: Monteiro OP]]
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[[Category: Monteiro, O P.]]
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[[Category: Picaud S]]
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[[Category: Picaud, S.]]
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[[Category: Von Delft F]]
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[[Category: SGC, Structural Genomics Consortium.]]
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[[Category: Bromodomain]]
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[[Category: Creb binding]]
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[[Category: Crebbp]]
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[[Category: Kat3a]]
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[[Category: Rst]]
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[[Category: Rst]]
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[[Category: Sgc]]
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[[Category: Structural genomics consortium]]
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[[Category: Transcription]]
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Current revision

Crystal Structure of the Bromodomain of human CREBBP in complex with a quinazolin-one ligand

PDB ID 4nyv

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