Literature DB >> 6331440

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

A Minocha, B H Long.   

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.

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Year:  1984        PMID： 6331440     DOI： 10.1016/0006-291x(84)90454-6

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN： 0006-291X            Impact factor:   3.575


  20 in total

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Review 9.  Pharmacokinetic optimisation of treatment with oral etoposide.

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10.  Estrogen treatment induces MLL aberrations in human lymphoblastoid cells.

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