4nr5

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{{STRUCTURE_4nr5| PDB=4nr5 | SCENE= }}
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==Crystal structure of the bromodomain of human CREBBP in complex with an isoxazolyl-benzimidazole ligand==
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===Crystal structure of the bromodomain of human CREBBP in complex with an isoxazolyl-benzimidazole ligand===
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<StructureSection load='4nr5' size='340' side='right' caption='[[4nr5]], [[Resolution|resolution]] 1.66&Aring;' scene=''>
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== Structural highlights ==
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==Disease==
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<table><tr><td colspan='2'>[[4nr5]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NR5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4NR5 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=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>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nr4|4nr4]], [[4nr6|4nr6]], [[4nr7|4nr7]]</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CBP, CREBBP ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=4nr5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nr5 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4nr5 RCSB], [http://www.ebi.ac.uk/pdbsum/4nr5 PDBsum]</span></td></tr>
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</table>
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== Disease ==
[[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>
[[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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==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>
[[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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==About this Structure==
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==See Also==
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[[4nr5]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NR5 OCA].
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*[[CREB-binding protein|CREB-binding protein]]
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== References ==
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==Reference==
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<references/>
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<references group="xtra"/><references/>
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__TOC__
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</StructureSection>
[[Category: Histone acetyltransferase]]
[[Category: Histone acetyltransferase]]
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[[Category: Arrowsmith, C H.]]
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[[Category: Human]]
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[[Category: Bountra, C.]]
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[[Category: Arrowsmith, C H]]
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[[Category: Brennan, P.]]
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[[Category: Bountra, C]]
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[[Category: Delft, F Von.]]
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[[Category: Brennan, P]]
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[[Category: Edwards, A M.]]
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[[Category: Delft, F Von]]
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[[Category: Fedorov, O.]]
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[[Category: Edwards, A M]]
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[[Category: Felletar, I.]]
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[[Category: Fedorov, O]]
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[[Category: Filippakopoulos, P.]]
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[[Category: Felletar, I]]
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[[Category: Hay, D.]]
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[[Category: Filippakopoulos, P]]
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[[Category: Knapp, S.]]
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[[Category: Hay, D]]
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[[Category: Martin, S.]]
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[[Category: Knapp, S]]
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[[Category: Picaud, S.]]
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[[Category: Martin, S]]
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[[Category: Pike, A W.]]
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[[Category: Picaud, S]]
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[[Category: SGC, Structural Genomics Consortium.]]
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[[Category: Pike, A W]]
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[[Category: Structural genomic]]
[[Category: Chemical tool]]
[[Category: Chemical tool]]
[[Category: Sgc]]
[[Category: Sgc]]
[[Category: Small molecule inhibitor]]
[[Category: Small molecule inhibitor]]
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[[Category: Structural genomics consortium]]
 
[[Category: Transcription]]
[[Category: Transcription]]
[[Category: Transcription-inhibitor complex]]
[[Category: Transcription-inhibitor complex]]

Revision as of 16:52, 21 December 2014

Crystal structure of the bromodomain of human CREBBP in complex with an isoxazolyl-benzimidazole ligand

4nr5, resolution 1.66Å

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