Dual Inhibitors of Human DNA Topoisomerase II and Other Cancer-Related Targets.,Journal of Medicinal Chemistry

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Dual Inhibitors of Human DNA Topoisomerase II and Other Cancer-Related Targets.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-10-21 , DOI: 10.1021/acs.jmedchem.9b00726
Žiga Skok ₁ , Nace Zidar ₁ , Danijel Kikelj ₁ , Janez Ilaš ₁

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Human DNA topoisomerase II is an important target in anticancer therapy. Despite the clinical success of drugs that target topoisomerase II, the development of resistant cancer cells can limit their clinical efficacy. To maximize the therapeutic potential of anticancer drugs, combination therapies and multitarget drugs have been suggested in many studies, where the use of multitarget drugs is advantageous from a pharmacokinetic point of view. There are various different options for the preparation of dual-target or multiple-target inhibitors, as topoisomerase II is both structurally (e.g., topoisomerase I, Hsp90, and kinases) and functionally (e.g., histone deacetylases and proteasome) connected to many validated anticancer targets. In this Perspective, we discuss the scientific background behind targeting topoisomerase II together with a number of other targets important in cancer therapy, review the present status, and discuss further options in the field.

中文翻译：

人类DNA拓扑异构酶II和其他癌症相关靶标的双重抑制剂。

人DNA拓扑异构酶II是抗癌治疗中的重要靶标。尽管靶向拓扑异构酶II的药物在临床上取得了成功，但耐药性癌细胞的发展会限制其临床疗效。为了最大化抗癌药的治疗潜力，在许多研究中已经提出了联合疗法和多靶点药物，其中从药代动力学的角度来看，使用多靶点药物是有利的。制备双靶或多靶抑制剂有多种选择，因为拓扑异构酶II在结构上（例如拓扑异构酶I，Hsp90和激酶）在功能上（例如组蛋白脱乙酰酶和蛋白酶体）都与许多经过验证的抗癌药物相关目标。从这个角度来看，

更新日期：2019-10-21

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