Recent developments in topoisomerase-targeted cancer chemotherapy.
Recent developments in topoisomerase-targeted cancer chemotherapy.
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DOI：
10.1016/j.apsb.2018.07.008
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发表时间：
2018-10
期刊：
影响因子：
--
通讯作者：
Mooney JW
中科院分区：
文献类型：
--
作者：
Hevener K;Verstak TA;Lutat KE;Riggsbee DL;Mooney JW
DNA拓扑异构酶是细胞功能所必需的，并且在生命的所有领域中普遍存在。各种拓扑异构酶在DNA复制期间执行与DNA拓扑结构的维持相关的广泛功能，并且转录是广泛的抗微生物剂和癌症化疗剂的靶标。天然产物衍生的药物，如喜树碱、蒽环类药物和鬼臼毒素药物，已广泛用于治疗多种类型的癌症。选择性靶向拓扑异构酶用于癌症治疗仍然是基础和临床研究的一个高度活跃的领域。本综述的重点将是总结目前最先进的临床使用的拓扑异构酶抑制剂靶向治疗癌症，并讨论有前途的新的拓扑异构酶抑制剂在临床和临床前开发的药理学和化学。本文综述了拓扑异构酶为靶点的肿瘤治疗药物的研究现状。讨论了在临床试验和临床前开发中有前途的新型拓扑异构酶抑制剂的药理学和化学。重点放在抑制机制，异构体的选择性，和讨论的化合物的效力。
The DNA topoisomerase enzymes are essential to cell function and are found ubiquitously in all domains of life. The various topoisomerase enzymes perform a wide range of functions related to the maintenance of DNA topology during DNA replication, and transcription are the targets of a wide range of antimicrobial and cancer chemotherapeutic agents. Natural product-derived agents, such as the camptothecin, anthracycline, and podophyllotoxin drugs, have seen broad use in the treatment of many types of cancer. Selective targeting of the topoisomerase enzymes for cancer treatment continues to be a highly active area of basic and clinical research. The focus of this review will be to summarize the current state of the art with respect to clinically used topoisomerase inhibitors for targeted cancer treatment and to discuss the pharmacology and chemistry of promising new topoisomerase inhibitors in clinical and pre-clinical development. This review summarizes the current state of the art of topoisomerase-targeted drug discovery for cancer therapeutics. The pharmacology and chemistry of promising new topoisomerase inhibitors in clinical trials and pre-clinical development are discussed. Emphases are placed on inhibitory mechanism, isoform selectivity, and the potency of the compounds discussed.
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影响因子：
2.9
作者：
ALI, JA;JACKSON, AP;MAXWELL, A
通讯作者：
MAXWELL, A
影响因子：
3
作者：
Cuya, Selma M.;Bjornsti, Mary-Ann;van Waardenburg, Robert C. A. M.
通讯作者：
van Waardenburg, Robert C. A. M.
影响因子：
64.8
作者：
Berger, JM;Gamblin, SJ;Wang, JC
通讯作者：
Wang, JC
DOI：
10.1186/1472-6769-9-1
发表时间：
2009-01-07
期刊：
BMC chemical biology
影响因子：
--
作者：
通讯作者：
--
影响因子：
14.9
作者：
Baker NM;Rajan R;Mondragón A
通讯作者：
Mondragón A