4.5 Article

Mining for METTL3 inhibitors to suppress cancer

Journal

NATURE STRUCTURAL & MOLECULAR BIOLOGY
Volume 28, Issue 6, Pages 460-462

Publisher

NATURE PORTFOLIO
DOI: 10.1038/s41594-021-00606-5

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Funding

  1. National Cancer Institute (NCI) of the NIH [R35CA232115, R01CA233671]

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The RNA methyltransferase METTL3 plays a crucial role in cancer development and progression, particularly in AML. A selective small molecule inhibitor of METTL3 has shown promising antileukemic effects in preclinical models, suggesting a potential new cancer therapy targeting METTL3.
The RNA methyltransferase METTL3 catalyzes N-6-methyladenosine (m(6)A) 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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