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 anti-leukemic effects in preclinical AML models, highlighting the promise of pharmacological METTL3 inhibition as a new cancer therapy.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Binding Sites
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Cell Line, Tumor
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Drug Discovery / methods*
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Drug Screening Assays, Antitumor
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Hematopoietic Stem Cells / drug effects
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Humans
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Leukemia, Myeloid, Acute / drug therapy
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Leukemia, Myeloid, Acute / enzymology
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Mass Spectrometry / methods
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Methyltransferases / antagonists & inhibitors*
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Methyltransferases / chemistry
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Mice
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Models, Molecular
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Molecular Targeted Therapy
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Neoplasm Proteins / antagonists & inhibitors*
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Neoplasms / drug therapy*
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Neoplastic Stem Cells / drug effects
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Protein Conformation
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S-Adenosylhomocysteine / analysis
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Xenograft Model Antitumor Assays
Substances
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Neoplasm Proteins
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S-Adenosylhomocysteine
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Methyltransferases
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METTL3 protein, human