Inhibitors of histone demethylases

被引:78
作者
Lohse, Brian [1 ]
Kristensen, Jesper L. [1 ]
Kristensen, Line H. [1 ]
Agger, Karl [2 ,3 ]
Helin, Kristian [2 ,3 ]
Gajhede, Michael [1 ]
Clausen, Rasmus P. [1 ]
机构
[1] Univ Copenhagen, Dept Med Chem, Fac Pharmaceut Sci, DK-2100 Copenhagen, Denmark
[2] Univ Copenhagen, BRIC, DK-2200 Copenhagen, Denmark
[3] Univ Copenhagen, Ctr Epigenet, DK-2200 Copenhagen, Denmark
基金
新加坡国家研究基金会; 英国医学研究理事会;
关键词
Histone demethylases; Epigenetics; Inhibitors; HDM; LSD1; HYPOXIA-INDUCIBLE FACTOR; LYSINE-SPECIFIC DEMETHYLASE-1; MECHANISM-BASED INACTIVATOR; DOMAIN-CONTAINING PROTEINS; CRYSTAL-STRUCTURE; STRUCTURAL BASIS; SUBSTRATE-SPECIFICITY; INDUCED SENESCENCE; POLYAMINE OXIDASE; ANDROGEN-RECEPTOR;
D O I
10.1016/j.bmc.2011.01.046
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3625 / 3636
页数:12
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