KDM4 histone demethylase inhibitors for anti-cancer agents: a patent review

被引：30
作者：
Chin, Young-Won [1 ,2 ]
Han, Sun-Young [3 ,4 ]
机构：
[1] Dongguk Univ Seoul, Coll Pharm, Goyang 410820, Gyeonggi Do, South Korea
[2] Dongguk Univ Seoul, R FIND Team BK21PLUS, Goyang 410820, Gyeonggi Do, South Korea
[3] Gyeongsang Natl Univ, Coll Pharm, Jinju 660751, Gyeongnam, South Korea
[4] Gyeongsang Natl Univ, Life Sci Res Inst, Jinju 660751, Gyeongnam, South Korea
来源：
EXPERT OPINION ON THERAPEUTIC PATENTS | 2015年 / 25卷 / 02期
关键词：
epigenetics; histone demethylase; JHDM3; Jumonji D2; KDM4; JUMONJI C; JMJD2A; MODULATION; LYSINE-9; AMPLICON; ASSAYS; GASC1;
D O I：
10.1517/13543776.2014.991310
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Introduction: As epigenetic modulators, histone demethylases can be a therapeutic target in the area of oncology. KDM4 subfamily proteins are histone demethylases with a Jumonji domain. The subfamily consists of five functional members: KDM4A, KDM4B, KDM4C, KDM4D, and KDM4E. The role of the KDM4 subfamily proteins is reported in oncogenesis, and their overexpression in various tumor types is observed. Small molecule inhibitors for KDM4 proteins have great potential in anti-cancer therapy. Areas covered: A comprehensive review of the patents for KDM4 inhibitors is provided in this paper. Small molecule structural information and pharmacological effects are presented in the content. Expert opinion: The status of KDM4 inhibitor development is still in the early stages with small numbers of patents and journal articles. Future KDM4 inhibitor development should focus on obtaining selectivity between KDM4 subtypes, development of small molecules with in vivo activity, and extension of the therapeutic area of KDM4 inhibitors other than use in cancer therapy.
引用
收藏
页码：135 / 144
页数：10
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