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新药研发前沿动态 / 医药领域趋势进展

WANG Xianghan, XU Jun, FEI Wenlong, YOU Qidong, GUO Xiaoke. Progress of Small-Molecule Inhibitors of m6A Demethylases[J]. Progress in Pharmaceutical Sciences, 2023, 47(9): 665-681. DOI: 10.20053/j.issn1001-5094.2023.09.003
Citation: WANG Xianghan, XU Jun, FEI Wenlong, YOU Qidong, GUO Xiaoke. Progress of Small-Molecule Inhibitors of m6A Demethylases[J]. Progress in Pharmaceutical Sciences, 2023, 47(9): 665-681. DOI: 10.20053/j.issn1001-5094.2023.09.003

Progress of Small-Molecule Inhibitors of m6A Demethylases

  • N6-methyladenosine (m6A) is one of the most common and conservative modifications in RNA, and is also a hot target in epigenetics research. The m6A modification in mammalian is dynamic and reversible. The abnormality of m6A is related to the formation and development of many diseases. The m6A demethylation of RNA catalyzed by m6A demethylases, including fat mass and obesity-associated proteins (FTO), Alkb Homologue 5 (ALKBH5) and Alkb Homologue 3 (ALKBH3). Inhibition of m6A demethylase can regulate the level of m6A, reduce cell viability and inhibit tumor growth in associated cancers. The study of small molecule inhibitors targeting m6A demethylase has become a hot topic in the field of anti-tumor drug research. This paper reviews the m6A demethylase related diseases such as cancer and the research progress of various small molecule inhibitors of m6A demethylases, which provides a basis for further research and development of related drugs.
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