Article
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
Nature - 6 Dec 2012
McCabe Michael T, Ott Heidi M, Ganji Gopinath, Korenchuk Susan, Thompson Christine, Van Aller Glenn S, Liu Yan, Graves Alan P, Della Pietra Anthony, Diaz Elsie, LaFrance Louis V, Mellinger Mark, Duquenne Celine, Tian Xinrong, Kruger Ryan G, McHugh Charles F, Brandt Martin, Miller William H, Dhanak Dashyant, Verma Sharad K, Tummino Peter J, Creasy Caretha L
Abstract excerpt
In eukaryotes, post-translational modification of histones is critical for regulation of chromatin structure and gene expression. EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2) and is involved in repressing gene expression through methylation of histone H3 on lysine 27 (H3K27). EZH2 overexpression is implicated in tumorigenesis and correlates with poor prognosis in several tumour types....
Topics
- Animals
- Cell Line, Tumor
- Cell Proliferation
- Enhancer of Zeste Homolog 2 Protein
- Gene Expression Regulation, Neoplastic
- Gene Silencing
- Histone Methyltransferases
- Histone-Lysine N-Methyltransferase