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Mining for METTL3 inhibitors to suppress cancer

Authors
  • Li, Jiazhi1, 2
  • Gregory, Richard I.1, 2, 2, 3, 4
  • 1 Boston Children’s Hospital, Boston, MA, USA , Boston (United States)
  • 2 Harvard Medical School, Boston, MA, USA , Boston (United States)
  • 3 Harvard Stem Cell Institute, Cambridge, MA, USA , Cambridge (United States)
  • 4 Harvard Initiative for RNA Medicine, Boston, MA, USA , Boston (United States)
Type
Published Article
Journal
Nature Structural & Molecular Biology
Publisher
Springer Nature
Publication Date
May 26, 2021
Volume
28
Issue
6
Pages
460–462
Identifiers
DOI: 10.1038/s41594-021-00606-5
Source
Springer Nature
Disciplines
  • news-and-views
License
Yellow

Abstract

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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