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Identification of a Small-Molecule Inhibitor of DNA Topoisomerase II by Proteomic Profiling

Identification of a Small-Molecule Inhibitor of DNA Topoisomerase II by Proteomic Profiling

Makoto Kawatani, Hiroshi Takayama, Makoto Muroi, Shinya Kimura, Taira Maekawa, Hiroyuki Osada

Chem Biol. 2011 Jun 24;18(6):743-51.

PMID: 21700210

Abstract:

BNS-22, a chemically synthesized derivative of the natural plant product GUT-70, has antiproliferative activity against human cancer cells, the mechanism of which is unknown. Here, we identify a target of BNS-22 by proteomic profiling analysis, which suggests that BNS-22 belongs to the same cluster as ICRF-193, a DNA topoisomerase II (TOP2) catalytic inhibitor. BNS-22 inhibits kinetoplast DNA decatenation that is mediated by human TOP2α and TOP2β in vitro at an IC(50) of 2.8 and 0.42 μM, respectively. BNS-22 does not affect DNA damage and antagonizes TOP2 poison-mediated DNA damage. Like ICRF-193, BNS-22 induces mitotic abnormalities, characterized by impairments in chromosome alignment and segregation, thereby causing polyploidy in HeLa cells. These results indicate that BNS-22 targets TOP2 and acts as its catalytic inhibitor.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1151668244	BNS-22		1151668-24-4	Price
IAR42415762	Topoisomerase II Inhibitor, BNS-22			Price

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