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引用次数: 0
摘要
拓扑异构酶是一种控制 DNA 链拓扑结构的无处不在的酶。人们对来自天然来源的拓扑异构酶抑制剂进行了广泛的研究，这些抑制剂可部分诱导肿瘤细胞凋亡。然而，这些抑制剂在治疗肝细胞癌方面的具体疗效还相对欠缺。因此，本综述将重点关注肝细胞癌中拓扑异构酶抑制剂的结构特征和抗癌特性。此外，本综述还阐明了所述天然生物活性化合物的作用机制、结构-活性关系、治疗局限性、临床试验阶段及其在癌症化疗中的潜在应用。对拓扑异构酶医学生物学的广泛了解将为提高合理抗肝细胞癌药物发现的效率提供不可或缺的框架。
Unravelling the role of natural and synthetic products as DNA topoisomerase inhibitors in hepatocellular carcinoma.
Topoisomerase is a ubiquitous enzyme in the control of DNA chain topology. There have been extensive research on topoisomerase inhibitors derived from natural sources, which act as partial inducers of tumor cell apoptosis. However, their specific efficacy in treating hepatocellular carcinoma is relatively unexplored. Hence, this comprehensive review focuses on the structural characteristics and anti-cancer properties of topoisomerase inhibitors in hepatocellular carcinoma. Furthermore, this review is also elucidating the mechanism of action, structure-activity relationships, therapeutic limitations, stage of clinical trials of described classes of natural bioactive compounds as well as their potential application in cancer chemotherapies. This broad understanding of topoisomerase medical biology will provide indispensable framework for enhancing the efficiency of rational anti-hepatocellular carcinoma drug discovery.
期刊介绍：
Bioorganic Chemistry publishes research that addresses biological questions at the molecular level, using organic chemistry and principles of physical organic chemistry. The scope of the journal covers a range of topics at the organic chemistry-biology interface, including: enzyme catalysis, biotransformation and enzyme inhibition; nucleic acids chemistry; medicinal chemistry; natural product chemistry, natural product synthesis and natural product biosynthesis; antimicrobial agents; lipid and peptide chemistry; biophysical chemistry; biological probes; bio-orthogonal chemistry and biomimetic chemistry.
For manuscripts dealing with synthetic bioactive compounds, the Journal requires that the molecular target of the compounds described must be known, and must be demonstrated experimentally in the manuscript. For studies involving natural products, if the molecular target is unknown, some data beyond simple cell-based toxicity studies to provide insight into the mechanism of action is required. Studies supported by molecular docking are welcome, but must be supported by experimental data. The Journal does not consider manuscripts that are purely theoretical or computational in nature.
The Journal publishes regular articles, short communications and reviews. Reviews are normally invited by Editors or Editorial Board members. Authors of unsolicited reviews should first contact an Editor or Editorial Board member to determine whether the proposed article is within the scope of the Journal.
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