Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer.
Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer.
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DOI：
10.3390/cancers3011383
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发表时间：
2011-03-01
期刊：
影响因子：
5.2
通讯作者：
Yan Q
中科院分区：
文献类型：
--
作者：
Blair LP;Cao J;Zou MR;Sayegh J;Yan Q
与遗传改变相似，表观遗传畸变对肿瘤的发生和进展有重要作用。在许多情况下，这些变化是由维持表观遗传状态的调节因子的激活或失活引起的。在这里，我们回顾我们目前的知识KDM 5/JARID 1家族的组蛋白去甲基化酶。该酶家族包含JmjC结构域，并且能够从组蛋白H3上的赖氨酸4去除三甲基和二甲基标记。在这些蛋白质中，RBP 2介导耐药性，而JARID 1B是黑色素瘤维持所必需的。临床前研究表明，抑制这些酶可以抑制肿瘤发生，并为开发其抑制剂用于癌症治疗提供了强有力的理论基础。
Similar to genetic alterations, epigenetic aberrations contribute significantly to tumor initiation and progression. In many cases, these changes are caused by activation or inactivation of the regulators that maintain epigenetic states. Here we review our current knowledge on the KDM5/JARID1 family of histone demethylases. This family of enzymes contains a JmjC domain and is capable of removing tri- and di- methyl marks from lysine 4 on histone H3. Among these proteins, RBP2 mediates drug resistance while JARID1B is required for melanoma maintenance. Preclinical studies suggest inhibition of these enzymes can suppress tumorigenesis and provide strong rationale for development of their inhibitors for use in cancer therapy.