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Topoisomerase as target for antibacterial and anticancer drug discovery

机译:拓扑异构酶作为抗菌和抗癌药物发现的靶标

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摘要

DNA topoisomerases comprise a major aspect of basic cellular biology and are molecular targets for a variety of drugs like antibiotics, antibacterials and anticancer drugs. They act by inhibiting the topoisomerase molecule from relegating DNA strands after cleavage and convert the topoisomerases molecule into a DNA damaging agent. Though drugs of various categories acting through different mechanisms are available for the treatment, there are still problems associated with the currently available drugs. Therefore, Structural biologists, Structural chemists and Medicinal chemists all around the world have been identifying, designing, synthesizing and evaluating a variety of novel bioactive molecules targeting topoisomerase. This review summarizes types of topoisomerase and drug treating each class along with their structural requirement and activity. The emphasis has been laid in particular on the new potential heterocyles and the possible treatments as well as the current ongoing research status in the field of topoisomerase as dual targeting.
机译:DNA拓扑异构酶包含碱性细胞生物学的主要方面,是各种药物等抗生素,抗菌和抗癌药物的分子靶标。它们通过抑制在切割后从降级DNA链中抑制拓扑异构酶分子并将拓扑异构酶分子转化为DNA损伤剂。虽然通过不同机制的各种类别的药物可用于治疗,但仍有与目前可用的药物相关的问题。因此,世界各地的结构生物学家,结构化学家和药用化学家已经识别,设计,合成和评估靶向拓扑异构酶的各种新型生物活性分子。本综述总结了拓扑异构酶和药物处理每个阶级的类型以及它们的结构要求和活动。重点是新的潜在的超胶体和可能的治疗以及可能的治疗方法,以及拓扑异构酶领域的当前正在进行的研究状态作为双重靶向。

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