A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

Protein lysine methyltransferases G9a and GLP modulate the transcriptional repression of a variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as dimethylation of non-histone targets. Here we report the discovery of UNC0638, an inhibitor of G9a and GLP with excellent potency a...

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Autori principali: Vedadi, Masoud, Barsyte-Lovejoy, Dalia, Liu, Feng, Rival-Gervier, Sylvie, Allali-Hassani, Abdellah, Labrie, Viviane, Wigle, Tim J, Dimaggio, Peter A, Wasney, Gregory A, Siarheyeva, Alena, Dong, Aiping, Tempel, Wolfram, Wang, Sun-Chong, Chen, Xin, Chau, Irene, Mangano, Thomas J, Huang, Xi-ping, Simpson, Catherine D, Pattenden, Samantha G, Norris, Jacqueline L, Kireev, Dmitri B, Tripathy, Ashutosh, Edwards, Aled, Roth, Bryan L, Janzen, William P, Garcia, Benjamin A, Petronis, Arturas, Ellis, James, Brown, Peter J, Frye, Stephen V, Arrowsmith, Cheryl H, Jin, Jian
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2011
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3184254/
https://ncbi.nlm.nih.gov/pubmed/21743462
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nchembio.599
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