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氯喹喔啉磺酰胺(NSC 339004)是一种拓扑异构酶IIα/β毒药。

Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison.

作者信息

Gao H, Yamasaki E F, Chan K K, Shen L L, Snapka R M

机构信息

Department of Radiology, College of Medicine, Ohio State University, Columbus 43210, USA.

出版信息

Cancer Res. 2000 Nov 1;60(21):5937-40.

Abstract

Chloroquinoxaline sulfonamide (chlorosulfaquinoxaline, CQS, NSC 339004) is active against murine and human solid tumors. On the basis of its structural similarity to the topoisomerase IIbeta-specific drug XK469, CQS was tested and found to be both a topoisomerase-IIalpha and a topoisomerase-IIbeta poison. Topoisomerase II poisoning by CQS is essentially undetectable in assays using the common protein denaturant SDS, but easily detectable with strong chaotropic protein denaturants. The finding that detection of topoisomerase poisoning can be so dependent on the protein denaturant used in the assay has implications for drug discovery efforts and for our understanding of topoisomerase poisons.

摘要

氯喹喔啉磺酰胺(氯磺喹喔啉,CQS,NSC 339004)对小鼠和人类实体瘤具有活性。基于其与拓扑异构酶IIβ特异性药物XK469的结构相似性,对CQS进行了测试,发现它既是拓扑异构酶-IIα毒药,也是拓扑异构酶-IIβ毒药。在使用常见蛋白质变性剂SDS的检测中,基本上无法检测到CQS对拓扑异构酶II的毒害作用,但使用强离液序列高的蛋白质变性剂则很容易检测到。拓扑异构酶毒害作用的检测如此依赖于检测中使用的蛋白质变性剂这一发现,对药物研发工作以及我们对拓扑异构酶毒药的理解都有影响。

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