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Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes.

Abstract:

Centrosomes associate with spindle poles; thus, the presence of two centrosomes promotes bipolar spindle assembly in normal cells. Cancer cells often contain supernumerary centrosomes, and to avoid multipolar mitosis and cell death, these are clustered into two poles by the microtubule motor protein HSET. We report the discovery of an allosteric inhibitor of HSET, CW069, which we designed using a methodology on an interface of chemistry and biology. Using this approach, we explored millions o...

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Publication status:
Published

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Authors


Richards, FM More by this author
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Journal:
Chemistry and biology
Volume:
20
Issue:
11
Pages:
1399-1410
Publication date:
2013-11-05
DOI:
EISSN:
1879-1301
ISSN:
1074-5521
URN:
uuid:730ded60-d80a-4eca-9d53-2bd9f7f00713
Source identifiers:
438889
Local pid:
pubs:438889

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