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.
This is a preview of subscription content, access via your institution
Open Access articles citing this article.
Experimental Hematology & Oncology Open Access 21 February 2023
Cancer Cell International Open Access 11 December 2021
Access Nature and 54 other Nature Portfolio journals
Get Nature+, our best-value online-access subscription
$29.99 / 30 days
cancel any time
Subscribe to this journal
Receive 12 print issues and online access
$189.00 per year
only $15.75 per issue
Rent or buy this article
Prices vary by article type
Prices may be subject to local taxes which are calculated during checkout
Morera, L., Lübbert, M. & Jung, M. Clin. Epigenetics 8, 57 (2016).
Dominissini, D. et al. Nature 485, 201–206 (2012).
Meyer, K. D. et al. Cell 149, 1635–1646 (2012).
Meyer, K. D. & Jaffrey, S. R. Nat. Rev. Mol. Cell Biol. 15, 313–326 (2014).
Lin, S., Choe, J., Du, P., Triboulet, R. & Gregory, R. I. Mol. Cell 62, 335–345 (2016).
Choe, J. et al. Nature 561, 556–560 (2018).
Vu, L. P. et al. Nat. Med. 23, 1369–1376 (2017).
Barbieri, I. et al. Nature 552, 126–131 (2017).
Yankova, E. et al. Nature https://doi.org/10.1038/s41586-021-03536-w (2021).
Moroz-Omori, E. V. Preprint at bioRxiv https://doi.org/10.1101/2020.09.25.311803 (2020).
Wang, X. et al. Nature 505, 117–120 (2014).
Zaccara, S. & Jaffrey, S. R. Cell 181, 1582–1595.e18 (2020).
Paris, J. et al. Cell Stem Cell 25, 137–148.e6 (2019).
Li, Z. et al. Cancer Cell 31, 127–141 (2017).
Huang, Y. et al. Cancer Cell 35, 677–691.e10 (2019).
Shen, C. et al. Cell Stem Cell 27, 64–80.e9 (2020).
Mauer, J. et al. Nature 541, 371–375 (2017).
Mauer, J. et al. Nat. Chem. Biol. 15, 340–347 (2019).
R.I.G. is supported by an Outstanding Investigator Award (R35CA232115) and R01 grant (R01CA233671) from the National Cancer Institute (NCI) of the NIH.
R.I.G. is a cofounder and scientific advisory board member of 28-7 Therapeutics and Theon Therapeutics.
About this article
Cite this article
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
This article is cited by
Experimental Hematology & Oncology (2023)
Cancer Cell International (2021)