4nyw: Difference between revisions
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==Crystal Structure of the Bromodomain of human CREBBP in complex with a dihydroquinoxalinone ligand== | |||
<StructureSection load='4nyw' size='340' side='right' caption='[[4nyw]], [[Resolution|resolution]] 1.43Å' scene=''> | |||
== Structural highlights == | |||
==Disease== | <table><tr><td colspan='2'>[[4nyw]] 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=4NYW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4NYW FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2O3:(3R)-N-[3-(3,4-DIHYDROQUINOLIN-1(2H)-YL)PROPYL]-3-METHYL-2-OXO-1,2,3,4-TETRAHYDROQUINOXALINE-5-CARBOXAMIDE'>2O3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SCN:THIOCYANATE+ION'>SCN</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nyv|4nyv]], [[4nyx|4nyx]]</td></tr> | |||
<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> | |||
<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=4nyw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nyw OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4nyw RCSB], [http://www.ebi.ac.uk/pdbsum/4nyw PDBsum]</span></td></tr> | |||
</table> | |||
== 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> | ||
== Function == | |||
==Function== | |||
[[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> | ||
== | ==See Also== | ||
[[ | *[[CREB-binding protein|CREB-binding protein]] | ||
== References == | |||
== | <references/> | ||
<references | __TOC__ | ||
[[Category: Arrowsmith, C H | </StructureSection> | ||
[[Category: Bountra, C | [[Category: Human]] | ||
[[Category: Brennan, P | [[Category: Arrowsmith, C H]] | ||
[[Category: Conway, S J | [[Category: Bountra, C]] | ||
[[Category: Delft, F Von | [[Category: Brennan, P]] | ||
[[Category: Edwards, A M | [[Category: Conway, S J]] | ||
[[Category: Fedorov, O | [[Category: Delft, F Von]] | ||
[[Category: Felletar, I | [[Category: Edwards, A M]] | ||
[[Category: Filippakopoulos, P | [[Category: Fedorov, O]] | ||
[[Category: Knapp, S | [[Category: Felletar, I]] | ||
[[Category: Martin, S | [[Category: Filippakopoulos, P]] | ||
[[Category: Monteiro, O P | [[Category: Knapp, S]] | ||
[[Category: Picaud, S | [[Category: Martin, S]] | ||
[[Category: Rooney, T P.C | [[Category: Monteiro, O P]] | ||
[[Category: | [[Category: Picaud, S]] | ||
[[Category: Rooney, T P.C]] | |||
[[Category: Structural genomic]] | |||
[[Category: Bromodomain]] | [[Category: Bromodomain]] | ||
[[Category: Creb binding]] | [[Category: Creb binding]] | ||
[[Category: Crebbp]] | [[Category: Crebbp]] | ||
[[Category: Kat3a]] | [[Category: Kat3a]] | ||
[[Category: Rst]] | [[Category: Rst]] | ||
[[Category: Sgc]] | [[Category: Sgc]] | ||
[[Category: Transcription]] | [[Category: Transcription]] | ||
