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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 ACS+Med+Chem+Lett
2012 ; 3
(12
): 1091-6
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English Wikipedia
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine
Methyltransferase EZH2
#MMPMID24900432
Verma SK
; Tian X
; LaFrance LV
; Duquenne C
; Suarez DP
; Newlander KA
; Romeril SP
; Burgess JL
; Grant SW
; Brackley JA
; Graves AP
; Scherzer DA
; Shu A
; Thompson C
; Ott HM
; Aller GS
; Machutta CA
; Diaz E
; Jiang Y
; Johnson NW
; Knight SD
; Kruger RG
; McCabe MT
; Dhanak D
; Tummino PJ
; Creasy CL
; Miller WH
ACS Med Chem Lett
2012[Dec]; 3
(12
): 1091-6
PMID24900432
show ga
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.