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天仙丸对dna topoisomerases作用的研究

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中国肿瘤临床 1988年第6期15卷 340-341+2页

作者：李德华天津市医药科学研究所

本文证明天仙丸粗品的抗癌作用与其抑制人的dna Topoisomerase TypeⅡ有关,其T和9L 2个成分对dna Topoisomerase TypeⅠ和Type均有抑制作用。

关键词： dna topoisomerases 抑制作用所用抑制率粗品基因互作标准管

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Targeting Tyrosyl-dna phosphodiesterase I to enhance toxicity of phosphodiester linked dna-adducts

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Cancer Drug Resistance 2019年第4期2卷 1153-1163页

作者： Evan J.Brettrager Robert C.A.M.van Waardenburg Department of Pharmacology and Toxicology University of Alabama at BirminghamBirminghamAL 35294-0019USA

Our genomic dna is under constant assault from endogenous and exogenous sources,which needs to be resolved to maintain cellular homeostasis.The eukaryotic dna repair enzyme Tyrosyl-dna phosphodiesterase I(Tdp1)catalyzes the hydrolysis of phosphodiester bonds that covalently link adducts to dna-ends.Tdp1 utilizes two catalytic histidines to resolve a growing list of dna-adducts.These dna-adducts can be divided into two groups:small adducts,including oxidized nucleotides,RNA,and non-canonical nucleoside analogs,and large adducts,such as(drug-stabilized)topoisomerase-dna covalent complexes or failed Schiff base reactions as occur between PARP1 and dna.Many Tdp1 substrates are generated by chemotherapeutics linking Tdp1 to cancer drug resistance,making a compelling argument to develop small molecules that target Tdp1 as potential novel therapeutic agents.Tdp1’s unique catalytic cycle,which is centered on the formation of Tdp1-dna covalent reaction intermediate,allows for two principally different targeting strategies:(1)catalytic inhibition of Tdp1 catalysis to prevent Tdp1-mediated repair of dna-adducts that enhances the effectivity of chemotherapeutics;and(2)poisoning of Tdp1 by stabilization of the Tdp1-dna covalent reaction intermediate,which would increase the half-life of a potentially toxic dna-adduct by preventing its resolution,analogous to topoisomerase targeted poisons such as topotecan or etoposide.The catalytic Tdp1 mutant that forms the molecular basis of the autosomal recessive neurodegenerative disease spinocerebellar ataxia with axonal neuropathy best illustrates this concept;however,no small molecules have been reported for this strategy.Herein,we concisely discuss the development of Tdp1 catalytic inhibitors and their results.

关键词： Tdp1 small molecules dna topoisomerases Camptothecins oxidative dna damage dna adducts Etoposide chain terminating nucleotides/nucleoside analogs dna metabolism drug development

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A dual inhibitor of topoisomerases Ⅰ and Ⅱ of [(Ru(bpy)2(p-pippp)]2+

A dual inhibitor of topoisomerases Ⅰ and Ⅱ of [(Ru(bpy)2(p...

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第十一届全国化学生物学学术会议

作者： Jun-Feng Kou Han Zhu De-Chao Yang Feng-Yi Liu College of Chemistry and Chemical Engineering Yunnan Normal University

dna topoisomerases are essential enzymes that control and modify the topological states of dna.In accordance,topoisomerase activities are activated in cancer cell growths,and thus are important cellular targets for antineoplastic drugs.Ru(Ⅱ) complexes with polypyridyl ligands,due to a combination of easily constructed rigid chiral structures spanning all three spatial dimensions and a rich photophysical repertoire,have prominent dna binding properties. In order to obtain more insights into the topoisomerases inhibition of ruthenium(Ⅱ) complexes,a new mononuclear Ruthenium(Ⅱ)complex [(Ru(bpy)(p-pippp)] was synthesized and characterized by elemental analysis,ES-MS,1 HMNR.The dna-binding behaviors,dna topoisomerases inhibitory activities,antitumor activities and cell apoptosis in vitro were assessed.These results show the Ru(Ⅱ) complex acted as an efficient dual inhibitor of topoisomerases I and Ⅱ and good antitumor activities.

关键词： dna topoisomerases ruthenium（Ⅱ） complexes inhibitor antitumor activities

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