3p8h

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[[Image:3p8h.png|left|200px]]
 
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==Crystal structure of L3MBTL1 (MBT repeat) in complex with a nicotinamide antagonist==
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The line below this paragraph, containing "STRUCTURE_3p8h", creates the "Structure Box" on the page.
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<StructureSection load='3p8h' size='340' side='right'caption='[[3p8h]], [[Resolution|resolution]] 2.55&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3p8h]] 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=3P8H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3P8H 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]] 2.55&#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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=P8H:3-BROMO-5-[(4-PYRROLIDIN-1-YLPIPERIDIN-1-YL)CARBONYL]PYRIDINE'>P8H</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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{{STRUCTURE_3p8h| PDB=3p8h | SCENE= }}
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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=3p8h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3p8h OCA], [https://pdbe.org/3p8h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3p8h RCSB], [https://www.ebi.ac.uk/pdbsum/3p8h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3p8h ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/LMBL1_HUMAN LMBL1_HUMAN] Polycomb group (PcG) protein that specifically recognizes and binds mono- and dimethyllysine residues on target proteins, therey acting as a 'reader' of a network of post-translational modifications. PcG proteins maintain the transcriptionally repressive state of genes: acts as a chromatin compaction factor by recognizing and binding mono- and dimethylated histone H1b/HIST1H1E at 'Lys-26' (H1bK26me1 and H1bK26me2) and histone H4 at 'Lys-20' (H4K20me1 and H4K20me2), leading to condense chromatin and repress transcription. Recognizes and binds p53/TP53 monomethylated at 'Lys-382', leading to repress p53/TP53-target genes. Also recognizes and binds RB1/RB monomethylated at 'Lys-860'. Participates in the ETV6-mediated repression. Probably plays a role in cell proliferation. Overexpression induces multinucleated cells, suggesting that it is required to accomplish normal mitosis.<ref>PMID:17540172</ref> <ref>PMID:18408754</ref> <ref>PMID:20870719</ref> <ref>PMID:20870725</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Proteins which bind methylated lysines ("readers" of the histone code) are important components in the epigenetic regulation of gene expression and can also modulate other proteins that contain methyl-lysine such as p53 and Rb. Recognition of methyl-lysine marks by MBT domains leads to compaction of chromatin and a repressed transcriptional state. Antagonists of MBT domains would serve as probes to interrogate the functional role of these proteins and initiate the chemical biology of methyl-lysine readers as a target class. Small-molecule MBT antagonists were designed based on the structure of histone peptide-MBT complexes and their interaction with MBT domains determined using a chemiluminescent assay and ITC. The ligands discovered antagonize native histone peptide binding, exhibiting 5-fold stronger binding affinity to L3MBTL1 than its preferred histone peptide. The first cocrystal structure of a small molecule bound to L3MBTL1 was determined and provides new insights into binding requirements for further ligand design.
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===Crystal structure of L3MBTL1 (MBT repeat) in complex with a nicotinamide antagonist===
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Small-molecule ligands of methyl-lysine binding proteins.,Herold JM, Wigle TJ, Norris JL, Lam R, Korboukh VK, Gao C, Ingerman LA, Kireev DB, Senisterra G, Vedadi M, Tripathy A, Brown PJ, Arrowsmith CH, Jin J, Janzen WP, Frye SV J Med Chem. 2011 Apr 14;54(7):2504-11. Epub 2011 Mar 18. PMID:21417280<ref>PMID:21417280</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3p8h" style="background-color:#fffaf0;"></div>
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(as it appears on PubMed at http://www.pubmed.gov), where 21417280 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_21417280}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[3p8h]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3P8H OCA].
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==Reference==
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<ref group="xtra">PMID:021417280</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Arrowsmith, C H.]]
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[[Category: Large Structures]]
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[[Category: Bountra, C.]]
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[[Category: Arrowsmith CH]]
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[[Category: Brown, P J.]]
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[[Category: Bountra C]]
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[[Category: Edwards, A M.]]
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[[Category: Brown PJ]]
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[[Category: Frye, S V.]]
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[[Category: Edwards AM]]
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[[Category: Gao, C.]]
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[[Category: Frye SV]]
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[[Category: Herold, J M.]]
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[[Category: Gao C]]
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[[Category: Kireev, D.]]
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[[Category: Herold JM]]
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[[Category: Lam, R.]]
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[[Category: Kireev D]]
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[[Category: Ouyang, H.]]
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[[Category: Lam R]]
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[[Category: Ravichandran, M.]]
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[[Category: Ouyang H]]
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[[Category: SGC, Structural Genomics Consortium.]]
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[[Category: Ravichandran M]]
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[[Category: Senisterra, G.]]
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[[Category: Senisterra G]]
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[[Category: Tempel, W.]]
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[[Category: Tempel W]]
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[[Category: Vedadi, M.]]
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[[Category: Vedadi M]]
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[[Category: Weigelt, J.]]
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[[Category: Weigelt J]]

Current revision

Crystal structure of L3MBTL1 (MBT repeat) in complex with a nicotinamide antagonist

PDB ID 3p8h

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