Investigation of the biological mode of action of clerocidin using whole cell assays

被引：22

作者：

Jamora, C

Theodoraki, MA

Malhotra, V

Theodorakis, EA

机构：

[1] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA

[2] Univ Calif San Diego, Dept Biol, La Jolla, CA 92093 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 06期

关键词：

D O I：

10.1016/S0968-0896(01)00051-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Clerocidin, a diterpenoid natural product, has been shown in vitro to inhibit DNA religation following cleavage by topoisomerase II. Herein, we characterize the efficacy and specificity of clerocidin in HeLa cells. Our results suggest that clerocidin recognizes topoisomerase II as its main intracellular target and binds to this enzyme prior to formation of the 'cleavable complex' with DNA. These pharmacological features attest to the promising chemotherapeutic potential of this natural product. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

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页码：1365 / 1370

页数：6

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