The future therapeutic potential of histone demethylases: A critical analysis.

Gioacchino Natoli, Giuseppe Testa, Francesca De Santa
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Abstract

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.

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组蛋白去甲基化酶的未来治疗潜力:一项关键分析。
组蛋白尾部的甲基化曾经被认为是一种不可逆的修饰,最近随着组蛋白去甲基化酶的发现而受到重视,这些酶能够响应发育或环境因素。对组蛋白修饰的动态特性的认识激发了人们对靶向组蛋白甲基化/去甲基化的药物可能为癌症、炎症和代谢紊乱提供治疗这一概念的兴趣。然而,针对组蛋白去甲基化的表观遗传疗法尚处于概念阶段。本文就组蛋白去甲基化酶及其作为治疗靶点的潜力进行综述。
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