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CANCER DRUG DISCOVERY

Mining for METTL3 inhibitors to suppress cancer

The RNA methyltransferase METTL3 catalyzes N6-methyladenosine (m6A) modification of messenger RNAs (mRNAs). It is overexpressed in many types of cancer, including acute myelogenous leukemia (AML), and promotes cancer cell growth and tumorigenicity. Now, a selective small molecule inhibitor of METTL3 shows significant antileukemic effects in preclinical AML models, highlighting the promise of pharmacological METTL3 inhibition as a new cancer therapy.

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Fig. 1: METTL3 inhibition is a promising therapy against AML.

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Acknowledgements

R.I.G. is supported by an Outstanding Investigator Award (R35CA232115) and R01 grant (R01CA233671) from the National Cancer Institute (NCI) of the NIH.

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J.L. and R.I.G. wrote the manuscript.

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Correspondence to Richard I. Gregory.

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R.I.G. is a cofounder and scientific advisory board member of 28-7 Therapeutics and Theon Therapeutics.

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Li, J., Gregory, R.I. Mining for METTL3 inhibitors to suppress cancer. Nat Struct Mol Biol 28, 460–462 (2021). https://doi.org/10.1038/s41594-021-00606-5

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