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

Masoud Vedadi,Dalia Barsyte-Lovejoy,Feng Liu,Sylvie Rival-Gervier,Abdellah Allali-Hassani,Viviane Labrie,Tim J. Wigle,Peter A. DiMaggio,Gregory A. Wasney,Alena Siarheyeva,Aiping Dong,Wolfram Tempel,Sun-Chong Wang,Xin Chen,Irene Chau,Thomas J. Mangano,Xi Ping Huang,Catherine Simpson,Samantha G. Pattenden,Jacqueline L. Norris,Dmitri Kireev,Ashutosh Tripathy,Aled Edwards,Bryan L. Roth,William P. Janzen,Benjamin A. Garcia,Arturas Petronis,James Ellis,Peter J. Brown,Stephen V. Frye,Cheryl H. Arrowsmith,Jian Jin

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

2011

Protein lysine methyltransferases modulate the activities of chromatin and non-chromatin proteins by specific methylation of lysine side chains. A large-scale structure-based design approach has yielded a new chemical probe that potently and selectively inhibits G9a and GLP methyltransferases in cells.

Keywords:

EHMT2
Biochemistry
Methylation
DNA methylation
Cancer cell
Lysine
Histone-Lysine N-Methyltransferase
Methyltransferase
Chromatin
Biology

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