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从硬币到癌症治疗:靶向人类拓扑异构酶的金、银和铜配合物。

From coins to cancer therapy: Gold, silver and copper complexes targeting human topoisomerases.

机构信息

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, CS, Italy.

Department of Science, University of Basilicata, 85100 Potenza, Italy.

出版信息

Bioorg Med Chem Lett. 2020 Feb 1;30(3):126905. doi: 10.1016/j.bmcl.2019.126905. Epub 2019 Dec 17.

Abstract

Cancer is a complex issue and, even though the prevention basics and therapy have been implemented, it is still the second leading death cause worldwide. With the hope to discover new powerful and safer molecules to fight cancer, many researchers focused their attention on metal-based compounds, starting from the most famous and successfully employed anticancer drug, i.e. cisplatin. The current article aims to report the most recent discoveries about the use of gold, silver and copper complexes as antitumor agents, highlighting their influences on important enzymes, namely human topoisomerases. The latter are fundamental for the cell life and, if overexpressed, strongly implicated in cancer onset and progression. The identification of lead complexes targeting human topoisomerases and gifted with the appropriate chemical and pharmacological properties represents a fecund starting point to obtain new and more effective anticancer molecules.

摘要

癌症是一个复杂的问题,尽管已经实施了预防基础知识和治疗方法,但它仍然是全球第二大主要死亡原因。为了发现新的强大且更安全的抗癌分子,许多研究人员将注意力集中在基于金属的化合物上,从最著名且成功应用的抗癌药物顺铂开始。本文旨在报告有关金、银和铜配合物作为抗肿瘤剂的最新发现,强调它们对重要酶(即人类拓扑异构酶)的影响。后者对细胞生命至关重要,如果过度表达,则与癌症的发生和进展密切相关。鉴定针对人类拓扑异构酶并具有适当化学和药理学特性的先导配合物是获得新的、更有效的抗癌分子的一个富有成效的起点。

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