6yik: Difference between revisions

New page: '''Unreleased structure''' The entry 6yik is ON HOLD Authors: Picaud, S., Brand, M., Tobias, K., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Conway, S., Filippakopoulos...
 
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'''Unreleased structure'''


The entry 6yik is ON HOLD
==Crystal structure of the CREBBP bromodomain in complex with a tetrahydroquinoxaline ligand==
<StructureSection load='6yik' size='340' side='right'caption='[[6yik]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[6yik]] is a 3 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=6YIK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6YIK 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]] 1.7&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=OSQ:(3~{R})-~{N}-[3-(3,4-dihydro-2~{H}-quinolin-1-yl)-2,2-bis(fluoranyl)propyl]-3-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-quinoxaline-5-carboxamide'>OSQ</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=6yik FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6yik OCA], [https://pdbe.org/6yik PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6yik RCSB], [https://www.ebi.ac.uk/pdbsum/6yik PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6yik 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>


Authors: Picaud, S., Brand, M., Tobias, K., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Conway, S., Filippakopoulos, P.
==See Also==
 
*[[CREB-binding protein 3D structures|CREB-binding protein 3D structures]]
Description: Crystal structure of the CREBBP bromodomain in complex with a tetrahydroquinoxaline ligand
== References ==
[[Category: Unreleased Structures]]
<references/>
[[Category: Arrowsmith, C.H]]
__TOC__
[[Category: Von Delft, F]]
</StructureSection>
[[Category: Tobias, K]]
[[Category: Homo sapiens]]
[[Category: Picaud, S]]
[[Category: Large Structures]]
[[Category: Conway, S]]
[[Category: Arrowsmith CH]]
[[Category: Filippakopoulos, P]]
[[Category: Bountra C]]
[[Category: Brand, M]]
[[Category: Brand M]]
[[Category: Edwards, A.M]]
[[Category: Conway S]]
[[Category: Bountra, C]]
[[Category: Edwards AM]]
[[Category: Filippakopoulos P]]
[[Category: Picaud S]]
[[Category: Tobias K]]
[[Category: Von Delft F]]

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