Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules.
Basic Information
ID: ALA3576785
Journal: J Med Chem
Title: Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules.
Authors: Mariani A, Bartoli A, Atwal M, Lee KC, Austin CA, Rodriguez R.
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.
CiteXplore: 25945730
DOI: 10.1021/acs.jmedchem.5b00473
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