Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
ACS Med Chem Lett
; 3(12): 1091-6, 2012 Dec 13.
Article
en En
| MEDLINE
| ID: mdl-24900432
ABSTRACT
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part of a drug discovery program targeting EZH2, we have identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 (3) and GSK343 (6). These compounds are small molecule chemical tools that would be useful to further explore the biology of EZH2.
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Banco de datos:
MEDLINE
Tipo de estudio:
Diagnostic_studies
Idioma:
En
Año:
2012
Tipo del documento:
Article