期刊
FUTURE MEDICINAL CHEMISTRY
卷 11, 期 8, 页码 901-921出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2018-0380
关键词
chemical probes; protein methyltransferases; small-molecule inhibitors; SMYD2; SMYD3; structure-based drug discovery
资金
- Italian Association for Cancer Research [19172]
- Oncopenta project of the University of Bologna - Regione Emilia Romagna
- ISOF-CNR
- Innovamol
Lysine methyltransferases SMYD2 and SMYD3 are involved in the epigenetic regulation of cell differentiation and functioning. Overexpression and deregulation of these enzymes have been correlated to the insurgence and progression of different tumors, making them promising molecular targets in cancer therapy even if their role in tumors is not yet fully understood. In this light, selective small-molecule inhibitors are required to fully understand and validate these enzymes, as this is a prerequisite for the development of successful targeted therapeutic strategies. The present review gives a systematic overview of the chemical probes developed to selectively target SMYD2 and SMYD3, with particular focus on the structural features important for high inhibitory activity, on the mode of inhibition and on the efficacy in cell-based and in in vivo models. [GRAPHICS] .
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