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4l59

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{{STRUCTURE_4l59| PDB=4l59 | SCENE= }}
 
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===Crystal structure of the 3-MBT repeat domain of L3MBTL3 and UNC2533 complex===
 
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==Function==
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==Crystal structure of the 3-MBT repeat domain of L3MBTL3 and UNC2533 complex==
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[[http://www.uniprot.org/uniprot/LMBL3_HUMAN LMBL3_HUMAN]] Putative Polycomb group (PcG) protein. PcG proteins maintain the transcriptionally repressive state of genes, probably via a modification of chromatin, rendering it heritably changed in its expressibility. Required for normal maturation of myeloid progenitor cells (By similarity).
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<StructureSection load='4l59' size='340' side='right'caption='[[4l59]], [[Resolution|resolution]] 2.29&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4l59]] is a 1 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=4L59 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4L59 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]] 2.29&#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=1VZ:4-(PYRROLIDIN-1-YL)-1-{4-[2-(PYRROLIDIN-1-YL)ETHYL]PHENYL}PIPERIDINE'>1VZ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4l59 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4l59 OCA], [https://pdbe.org/4l59 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4l59 RCSB], [https://www.ebi.ac.uk/pdbsum/4l59 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4l59 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/LMBL3_HUMAN LMBL3_HUMAN] Putative Polycomb group (PcG) protein. PcG proteins maintain the transcriptionally repressive state of genes, probably via a modification of chromatin, rendering it heritably changed in its expressibility. Required for normal maturation of myeloid progenitor cells (By similarity).
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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We recently reported the discovery of UNC1215, a potent and selective chemical probe for the L3MBTL3 methyllysine reader domain. In this article, we describe the development of structure-activity relationships (SAR) of a second series of potent L3MBTL3 antagonists which evolved from the structure of the chemical probe UNC1215. These compounds are selective for L3MBTL3 against a panel of methyllysine reader proteins, particularly the related MBT family proteins, L3MBTL1 and MBTD1. A co-crystal structure of L3MBTL3 and one of the most potent compounds suggests that the L3MBTL3 dimer rotates about the dimer interface to accommodate ligand binding.
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==About this Structure==
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The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.,Camerino MA, Zhong N, Dong A, Dickson BM, James LI, Baughman BM, Norris JL, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV Medchemcomm. 2013 Nov;4(11):1501-1507. doi: 10.1039/C3MD00197K. PMID:24466405<ref>PMID:24466405</ref>
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[[4l59]] 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=4L59 OCA].
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[[Category: Human]]
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Arrowsmith, C H.]]
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</div>
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[[Category: Baughman, B M.]]
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<div class="pdbe-citations 4l59" style="background-color:#fffaf0;"></div>
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[[Category: Bountra, C.]]
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== References ==
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[[Category: Brown, P J.]]
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<references/>
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[[Category: Camerino, M A.]]
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__TOC__
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[[Category: Dickson, B M.]]
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</StructureSection>
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[[Category: Dong, A.]]
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[[Category: Homo sapiens]]
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[[Category: Edwards, A M.]]
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[[Category: Large Structures]]
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[[Category: Frye, S V.]]
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[[Category: Arrowsmith CH]]
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[[Category: Graslund, S.]]
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[[Category: Baughman BM]]
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[[Category: James, L I.]]
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[[Category: Bountra C]]
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[[Category: Janzen, W P.]]
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[[Category: Brown PJ]]
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[[Category: Kireev, D B.]]
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[[Category: Camerino MA]]
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[[Category: Norris, J L.]]
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[[Category: Dickson BM]]
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[[Category: Ravichandran, M.]]
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[[Category: Dong A]]
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[[Category: SGC, Structural Genomics Consortium.]]
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[[Category: Edwards AM]]
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[[Category: Zhong, N.]]
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[[Category: Frye SV]]
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[[Category: 3-mbt repeat domain]]
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[[Category: Graslund S]]
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[[Category: L3mbtl3]]
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[[Category: James LI]]
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[[Category: Sgc]]
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[[Category: Janzen WP]]
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[[Category: Structural genomic]]
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[[Category: Kireev DB]]
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[[Category: Structural genomics consortium]]
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[[Category: Norris JL]]
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[[Category: Transcription]]
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[[Category: Ravichandran M]]
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[[Category: Unc2533]]
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[[Category: Zhong N]]

Current revision

Crystal structure of the 3-MBT repeat domain of L3MBTL3 and UNC2533 complex

PDB ID 4l59

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