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Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules.

Abstract：

:The TOP2 poison etoposide has been implicated in the generation of secondary malignancies during cancer treatment. Structural similarities between TOP2 isoforms challenge the rational design of isoform-specific poisons to further delineate these processes. Herein, we describe the synthesis and biological evaluation of a focused library of etoposide analogues, with the identification of two novel small molecules exhibiting TOP2B-dependent toxicity. Our findings pave the way toward studying isoform-specific cellular processes by means of small molecule intervention.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Mariani A,Bartoli A,Atwal M,Lee KC,Austin CA,Rodriguez R

doi

10.1021/acs.jmedchem.5b00473

subject

Has Abstract

pub_date

2015-06-11 00:00:00

pages

4851-6

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章

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