期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 7, 页码 2103-2105出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.069
关键词
Protein arginine methyltransferases; Small-molecule inhibitors; S-Adenosylmethionine; Methylation; Epigenetics
资金
- Medical Research Council [G0700840]
- University of Nottingham
- MRC [G0700840] Funding Source: UKRI
- Medical Research Council [G0700840] Funding Source: researchfish
Prototype inhibitors of protein arginine methyltransferases (PRMTs) have been constructed by attaching guanidine functionality via a variable linker to non-reactive amine analogues of the cellular co-factor (S)-adenosyl methionine (AdoMet). Potent inhibition of PRMT1 (IC50 of similar to 3-6 mu M) combined with weak inhibition of the lysine methyltransferase SET7 (similar to 50% of activity at 100 mu M) was observed for two such compounds. (C) 2010 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据