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5ktw

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(New page: '''Unreleased structure''' The entry 5ktw is ON HOLD Authors: Murray, J.M., Boenig, G. Description: CREBBP bromodomain in complex with Cpd 44 (3-((5-acetyl-1-(cyclopropylmethyl)-4,5,6,...)
Current revision (12:42, 6 March 2024) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 5ktw is ON HOLD
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==CREBBP bromodomain in complex with Cpd 44 (3-((5-acetyl-1-(cyclopropylmethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)amino)-N-isopropylbenzamide)==
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<StructureSection load='5ktw' size='340' side='right'caption='[[5ktw]], [[Resolution|resolution]] 1.09&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5ktw]] 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=5KTW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5KTW FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.087&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6XG:3-[[1-(CYCLOPROPYLMETHYL)-5-ETHANOYL-6,7-DIHYDRO-4~{H}-PYRAZOLO[4,3-C]PYRIDIN-3-YL]AMINO]-~{N}-PROPAN-2-YL-BENZAMIDE'>6XG</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5ktw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ktw OCA], [https://pdbe.org/5ktw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ktw RCSB], [https://www.ebi.ac.uk/pdbsum/5ktw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ktw ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[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>
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== Function ==
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[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>
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Authors: Murray, J.M., Boenig, G.
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==See Also==
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*[[CREB-binding protein 3D structures|CREB-binding protein 3D structures]]
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Description: CREBBP bromodomain in complex with Cpd 44 (3-((5-acetyl-1-(cyclopropylmethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)amino)-N-isopropylbenzamide)
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== References ==
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[[Category: Unreleased Structures]]
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<references/>
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[[Category: Boenig, G]]
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__TOC__
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[[Category: Murray, J.M]]
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Boenig G]]
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[[Category: Murray JM]]

Current revision

CREBBP bromodomain in complex with Cpd 44 (3-((5-acetyl-1-(cyclopropylmethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)amino)-N-isopropylbenzamide)

PDB ID 5ktw

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