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组蛋白去甲基酶抑制剂。

Inhibitors of histone demethylases.

机构信息

Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, 2 Universitetsparken, DK-2100 Copenhagen, Denmark.

出版信息

Bioorg Med Chem. 2011 Jun 15;19(12):3625-36. doi: 10.1016/j.bmc.2011.01.046. Epub 2011 Feb 1.

Abstract

Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published.

摘要

甲基化赖氨酸是重要的表观遗传标记。最近发现了参与去甲基化的酶,这些酶与癌症的发生和发展有关。尽管这些酶是相对较新发现的,但已经出现了许多抑制剂。大多数抑制剂要么是先前报道的相关酶抑制剂,要么是源自这些抑制剂的化合物。在选择性和效力方面的发展仍然很重要。已经发表了几篇关于开发功能测定法的报告。

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