组蛋白去乙酰化酶抑制剂治疗子宫内膜异位症

Xin Li, Xi-shi Liu, Sun-Wei Guo
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引用次数: 10

摘要

子宫内膜异位症是一种常见的妇科疾病,主要影响育龄妇女。其主要症状包括痛经、慢性盆腔疼痛和不孕症。迫切需要开发更有效的治疗方法,最好是提高安全性和成本。不幸的是,到目前为止,药物开发进展缓慢得令人沮丧。本文回顾了支持子宫内膜异位症是一种表观遗传疾病这一观点的已发表数据。列举了组蛋白去乙酰化酶抑制剂作为治疗子宫内膜异位症的理想特性,并列出了在临床试验中评估组蛋白去乙酰化酶的障碍。有人认为,从药物发现的角度来看,丙戊酸的再利用是合理的。最后,指出了需要进一步研究的领域。
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Histone deacetylase inhibitors as therapeutics for endometriosis
Endometriosis is a common gynecological disorder affecting mostly women of reproductive age. Its presenting symptoms include dysmenorrhea, chronic pelvic pain and infertility. There is a pressing need to develop more efficacious therapeutics, preferably with improved safety and cost profiles. Unfortunately, thus far the drug development progress has been frustratingly slow. In this article, published data in support of the notion that endometriosis is an epigenetic disease are reviewed. The desirable properties of histone deacetylase inhibitors as therapeutics for treating endometriosis are enumerated, and the obstacles in evaluating histone deacetylases in clinical trials are listed. It is argued that, from the drug discovery standpoint, repurposing of valproic acid is justifiable. Finally, the areas in need of further research are exposed.
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