4i9o

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{{STRUCTURE_4i9o| PDB=4i9o | SCENE= }}
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==Crystal Structure of GACKIX L664C Tethered to 1-10==
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===Crystal Structure of GACKIX L664C Tethered to 1-10===
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<StructureSection load='4i9o' size='340' side='right' caption='[[4i9o]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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{{ABSTRACT_PUBMED_23384013}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4i9o]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4I9O OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4I9O 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=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=KI1:1-{4-[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]-4-HYDROXYPIPERIDIN-1-YL}-3-SULFANYLPROPAN-1-ONE'>KI1</scene></td></tr>
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<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=MSE:SELENOMETHIONINE'>MSE</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Crebbp, Cbp ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])</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=4i9o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4i9o OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4i9o RCSB], [http://www.ebi.ac.uk/pdbsum/4i9o PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Like many coactivators, the GACKIX domain of the master coactivator CBP/p300 recognizes transcriptional activators of diverse sequence composition via dynamic binding surfaces. The conformational dynamics of GACKIX that underlie its function also render it especially challenging for structural characterization. We have found that the ligand discovery strategy of Tethering is an effective method for identifying small-molecule fragments that stabilize the GACKIX domain, enabling for the first time the crystallographic characterization of this important motif. The 2.0 A resolution structure of GACKIX complexed to a small molecule was further analyzed by molecular dynamics simulations, which revealed the importance of specific side-chain motions that remodel the activator binding site in order to accommodate binding partners of distinct sequence and size. More broadly, these results suggest that Tethering can be a powerful strategy for identifying small-molecule stabilizers of conformationally malleable proteins, thus facilitating their structural characterization and accelerating the discovery of small-molecule modulators.
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==Function==
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Ordering a Dynamic Protein Via a Small-Molecule Stabilizer.,Wang N, Majmudar CY, Pomerantz WC, Gagnon JK, Sadowsky JD, Meagher JL, Johnson TK, Stuckey JA, Brooks CL 3rd, Wells JA, Mapp AK J Am Chem Soc. 2013 Feb 22. PMID:23384013<ref>PMID:23384013</ref>
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[[http://www.uniprot.org/uniprot/CBP_MOUSE CBP_MOUSE]] 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 (By similarity).<ref>PMID:10207073</ref> <ref>PMID:11701890</ref> <ref>PMID:15220471</ref> <ref>PMID:16287980</ref>
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[4i9o]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4I9O OCA].
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</div>
==See Also==
==See Also==
*[[CREB-binding protein|CREB-binding protein]]
*[[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]]
[[Category: Mus musculus]]
[[Category: Mus musculus]]
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[[Category: Mapp, A K.]]
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[[Category: Mapp, A K]]
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[[Category: Meagher, J L.]]
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[[Category: Meagher, J L]]
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[[Category: Stuckey, J A.]]
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[[Category: Stuckey, J A]]
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[[Category: Wang, N.]]
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[[Category: Wang, N]]
[[Category: Kix domain]]
[[Category: Kix domain]]
[[Category: Transcriptional coactivator]]
[[Category: Transcriptional coactivator]]
[[Category: Transferase]]
[[Category: Transferase]]

Revision as of 12:18, 21 December 2014

Crystal Structure of GACKIX L664C Tethered to 1-10

4i9o, resolution 2.00Å

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