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

Nature.. 2014-04;  508(7459):222-7
Huber KV, Salah E, Radic B, Gridling M, Elkins JM, Stukalov A, Jemth AS, GöktÜrk C, Sanjiv K, Strömberg K, Pham T, Berglund UW, Colinge J, Bennett K1, Loizou JI, Helleday T, Knapp S, Superti-Furga G. CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, 1090 Vienna, Austria.
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摘要

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 growth of KRAS tumour cells, whereas MTH1 overexpression mitigated sensitivity towards SCH51344. Searching for more drug-like inhibitors, we identified the kinase inhibitor crizotinib as a nanomolar suppressor of MTH1 activity. ... More

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