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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on the storage and integration of epigenetic drug datasets that were obtained from laboratory experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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Resveratrol-induced gene expression profiles in human prostate cancer cells

Drug Name:Resveratrol
Drug Category:HDACi
Sample Type:human prostate cancer cells
Condition:healthy
Experiment Type:Expression profiling by array
Experiment Platform:GPL182 SHV;GPL2669 SHAA;GPL2832 SHU;GPL2947 SHAS;GPL3045 SHBG;GPL3284 SHCW;GPL3285 SHCT;GPL3484 JBB;GPL3485 SHAF
Description:We describe the discovery of UNC1215, a potent and selective chemical probe for the ethyllysine (Kme) reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors. UNC1215 binds L3MBTL3 with a Kd of 120 nM, competitively displacing mono- or dimethyl-lysine containing peptides, and is greater than 50-fold selective versus other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a novel 2:2 polyvalent mode of interaction. In cells, UNC1215 is non-toxic and binds directly to L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins and point mutants that disrupt the Kme binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215. Finally, UNC1215 demonstrates a novel Kme-dependent interaction of L3MBTL3 with BCLAF1, a protein implicated in DNA damage repair and apoptosis.
PubmedID:15767336
Citation:James LI;Barsyte-Lovejoy D;Zhong N;Krichevsky L;Korboukh VK;Herold JM;MacNevin CJ;Norris JL;Sagum CA;Tempel W;Marcon E;Guo H;Gao C;Huang XP;Duan S;Emili A;Greenblatt JF;Kireev DB;Jin J;Janzen WP;Brown PJ;Bedford MT;Arrowsmith CH ; Frye SV.Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91. doi: 10.1038/nchembio.1157.
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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on integrating epigenetic drug studies based Omics data from high through experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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©2016 Group of Computational Epigenomics and Bioinformatics, College of Life Science, Jilin Normal University, China

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