5i86: Difference between revisions

Line 1:

~~'''Unreleased structure'''~~

~~The entry~~ 5i86 is ~~ON HOLD until Paper Publication~~

==Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02778174==

~~Authors~~: ~~Jayaram~~, H., ~~Poy~~, F., ~~Setser~~, J.W., ~~Bellon~~, ~~S.F~~.

== Structural highlights ==

<table><tr><td colspan='2'>[[5i86]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I86 OCA]. For a guided tour on the structure components use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I86 FirstGlance].

~~Description~~: ~~Crystal structure~~ of the ~~bromodomain~~ of ~~human CREBBP bound to the benzodiazepinone G02778174~~

</td></tr><tr id='ligand'><td class="sblockLbl">[[Ligand|Ligands:]]</td><td class="sblockDat"><scene name='pdbligand=69A:(4R)-N-BENZYL-4-METHYL-2-OXO-2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE-6-CARBOXAMIDE'>69A</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SCN:THIOCYANATE+ION'>SCN</scene></td></tr>

[[Category: ~~Unreleased Structures~~]]

<tr id='related'><td class="sblockLbl">[[Related_structure|Related:]]</td><td class="sblockDat">[[5i83|5i83]], [[5i89|5i89]]</td></tr>

<tr id='resources'><td class="sblockLbl">Resources:</td><td class="sblockDat">[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5i86 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i86 OCA], [http://pdbe.org/5i86 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i86 RCSB], [http://www.ebi.ac.uk/pdbsum/5i86 PDBsum]</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>

== 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>

== References ==

__TOC__

</StructureSection>

[[Category: Bellon, S F]]

[[Category: Jayaram, H]]

[[Category: Poy, F]]

[[Category: ~~Jayaram~~, H]]

[[Category: Setser, J W]]

[[Category: ~~Bellon, S.F~~]]

[[Category: Bromodomain inhibitor]]

[[Category: ~~Setser, J.W~~]]

[[Category: Protein binding-inhibitor complex]]

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@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
-The entry 5i86 is ON HOLD  until Paper Publication
+==Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02778174==
+<StructureSection load='5i86' size='340' side='right' caption='[[5i86]], [[Resolution|resolution]] 1.05&Aring;' scene=''>
-Authors: Jayaram, H., Poy, F., Setser, J.W., Bellon, S.F.
+== Structural highlights ==
+<table><tr><td colspan='2'>[[5i86]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I86 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I86 FirstGlance]. <br>
-Description: Crystal structure of the bromodomain of human CREBBP bound to the benzodiazepinone G02778174
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=69A:(4R)-N-BENZYL-4-METHYL-2-OXO-2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE-6-CARBOXAMIDE'>69A</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SCN:THIOCYANATE+ION'>SCN</scene></td></tr>
-[[Category: Unreleased Structures]]
+<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5i83|5i83]], [[5i89|5i89]]</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=5i86 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i86 OCA], [http://pdbe.org/5i86 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i86 RCSB], [http://www.ebi.ac.uk/pdbsum/5i86 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>
+== 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>
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Bellon, S F]]
+[[Category: Jayaram, H]]
 [[Category: Poy, F]]
-[[Category: Jayaram, H]]
+[[Category: Setser, J W]]
-[[Category: Bellon, S.F]]
+[[Category: Bromodomain inhibitor]]
-[[Category: Setser, J.W]]
+[[Category: Protein binding-inhibitor complex]]