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Inhibition of the DNA catenation activity of type II topoisomerase by VP16-213 and VM26.

Abstract：

:Studies suggest that the anticancer drugs VP16-213 and VM26 produce cytotoxicity by inducing protein-associated DNA breakage in vivo through interaction with a yet unknown nuclear component. The effects of these drugs and their congeners on topoisomerase activities was investigated. VP16-213, VM26, and congeners active toward inducing DNA breaks also inhibited the catenation activity of eukaryote type II topoisomerase in vitro at very low drug concentrations. A structure-activity relationship was obtained for inhibition of catenation that parallels in vivo DNA breakage and cytotoxic activities. Type I topoisomerase activity was totally unaffected by these drugs.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Minocha A,Long BH

doi

10.1016/0006-291x(84)90454-6

subject

Has Abstract

pub_date

1984-07-18 00:00:00

pages

165-70

issue

1

eissn

0006-291X

issn

1090-2104

pii

0006-291X(84)90454-6

journal_volume

122

pub_type

杂志文章

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