Research on cancer epigenetics has flourished in the last decade. Nevertheless growing evidence point on the importance to understand the mechanisms by which epigenetic changes regulate the genesis and progression of cancer growth. Several epigenetic targets have been discovered and are currently under validation for new anticancer therapies. Drug discovery approaches aiming to target these epigenetic enzymes with small-molecules inhibitors have produced the first pre-clinical and clinical outcomes and many other compounds are now entering the pipeline as new candidate epidrugs. The most studied targets can be ascribed to histone deacetylases and DNA methyltransferases, although several other classes of enzymes are able to operate post-translational modifications to histone tails are also likely to represent new frontiers for therapeutic interventions. By acknowledging that the field of cancer epigenetics is evolving with an impressive rate of new findings, with this review we aim to provide a current overview of pre-clinical applications of smallmolecules for cancer pathologies, combining them with the current knowledge of epigenetic targets in terms of available structural data and drug design perspectives.

译文

过去十年间,关于癌症表观遗传学的研究蓬勃发展。然而,越来越多的证据表明,了解表观遗传变化调控癌症发生和发展的机制的重要性。已经发现了几种表观遗传学靶标,目前正在对新的抗癌疗法进行验证。旨在利用小分子抑制剂靶向这些表观遗传酶的药物发现方法已产生了首个临床前和临床结果,许多其他化合物现在正作为新的候选表观药物进入开发阶段。研究最多的靶标可归因于组蛋白脱乙酰基酶和DNA甲基转移酶,尽管其他几类酶能够对组蛋白尾巴进行翻译后修饰,也可能代表治疗干预的新领域。通过认识到癌症表观遗传学领域正在以惊人的新发现发展,本综述旨在提供小分子在临床上用于癌症病理学的最新临床应用概述,并将其与表观遗传学靶点的当前知识相结合。现有的结构数据和药物设计观点。

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