6dmk
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==A multiconformer ligand model of an isoxazolyl-benzimidazole ligand bound to the bromodomain of human CREBBP== | |
+ | <StructureSection load='6dmk' size='340' side='right'caption='[[6dmk]], [[Resolution|resolution]] 1.66Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[6dmk]] is a 1 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=6DMK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6DMK 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]] 1.66Å</td></tr> | ||
+ | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=2LL:5-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-1-[2-(MORPHOLIN-4-YL)ETHYL]-2-(2-PHENYLETHYL)-1H-BENZIMIDAZOLE'>2LL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NO3:NITRATE+ION'>NO3</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=6dmk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dmk OCA], [https://pdbe.org/6dmk PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6dmk RCSB], [https://www.ebi.ac.uk/pdbsum/6dmk PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6dmk 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> | ||
- | + | ==See Also== | |
- | + | *[[CREB-binding protein 3D structures|CREB-binding protein 3D structures]] | |
- | + | == References == | |
- | [[Category: | + | <references/> |
+ | __TOC__ | ||
+ | </StructureSection> | ||
+ | [[Category: Homo sapiens]] | ||
+ | [[Category: Large Structures]] | ||
+ | [[Category: Borrelli K]] | ||
+ | [[Category: Day T]] | ||
+ | [[Category: Fonseca R]] | ||
+ | [[Category: Fraser JS]] | ||
+ | [[Category: Heliou A]] | ||
+ | [[Category: Hudson BM]] | ||
+ | [[Category: Keedy D]] | ||
+ | [[Category: Suresh P]] | ||
+ | [[Category: Van Zundert G]] | ||
+ | [[Category: Van den Bedem H]] |
Current revision
A multiconformer ligand model of an isoxazolyl-benzimidazole ligand bound to the bromodomain of human CREBBP
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Categories: Homo sapiens | Large Structures | Borrelli K | Day T | Fonseca R | Fraser JS | Heliou A | Hudson BM | Keedy D | Suresh P | Van Zundert G | Van den Bedem H