Natoli Gioacchino, Testa Giuseppe, De Santa Francesca
European Institue of Oncology, Department of Experimental Oncology, Milan, Italy.
Curr Opin Drug Discov Devel. 2009 Sep;12(5):607-15.
Once regarded as an irreversible modification, the methylation of histone protein tails has recently been highlighted following the identification of enzymes capable of histone demethylation in response to developmental or environmental cues. An awareness of the dynamic nature of histone modification has stimulated interest in the concept that drugs targeting histone methylation/demethylation might provide treatments for cancer, inflammation and metabolic disorders. However, epigenetic therapies that target histone demethylation are at the concept stage. Histone demethylases and their potential as therapeutic targets are discussed in this review.
组蛋白尾部甲基化曾被视为一种不可逆的修饰，然而，随着能够响应发育或环境信号进行组蛋白去甲基化的酶被发现，最近它受到了关注。对组蛋白修饰动态特性的认识激发了人们对于靶向组蛋白甲基化/去甲基化的药物可能为癌症、炎症和代谢紊乱提供治疗方法这一概念的兴趣。然而，靶向组蛋白去甲基化的表观遗传疗法仍处于概念阶段。本文综述讨论了组蛋白去甲基化酶及其作为治疗靶点的潜力。
