4l59
From Proteopedia
(Difference between revisions)
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== Function == | == Function == | ||
[[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). | [[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). | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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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| + | 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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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 4l59" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Revision as of 05:42, 16 May 2018
Crystal structure of the 3-MBT repeat domain of L3MBTL3 and UNC2533 complex
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Categories: Human | Arrowsmith, C H | Baughman, B M | Bountra, C | Brown, P J | Camerino, M A | Dickson, B M | Dong, A | Edwards, A M | Frye, S V | Graslund, S | James, L I | Janzen, W P | Kireev, D B | Norris, J L | Ravichandran, M | Structural genomic | Zhong, N | 3-mbt repeat domain | L3mbtl3 | Sgc | Transcription | Unc2533
