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Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.

Abstract:

Activated RAS GTPase signalling is a critical driver of oncogenic transformation and malignant disease. Cellular models of RAS-dependent cancers have been used to identify experimental small molecules, such as SCH51344, but their molecular mechanism of action remains generally unknown. Here, using a chemical proteomic approach, we identify the target of SCH51344 as the human mutT homologue MTH1 (also known as NUDT1), a nucleotide pool sanitizing enzyme. Loss-of-function of MTH1 impaired growt...

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Publication status:
Published

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Publisher copy:
10.1038/nature13194

Authors


Gridling, M More by this author
Elkins, JM More by this author
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Journal:
Nature
Volume:
508
Issue:
7495
Pages:
222-227
Publication date:
2014-04-02
DOI:
EISSN:
1476-4687
ISSN:
0028-0836
URN:
uuid:28882238-b520-469b-8eb9-adce7a4ef327
Source identifiers:
458657
Local pid:
pubs:458657

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