Targeted Degradation of METTL3 Against Acute Myeloid Leukemia and Gastric Cancer
Kyubin Hwang,
Juhyeon Bae,
Yoo-Lim Jhe
et al.
Abstract:Accumulating evidence reveals the oncogenic role of methyltransferase-like 3 (METTL3) in a variety of cancer types, either dependent or independent of its m6A methyl transferase activity. We have designed proteolysis-targeting chimeras (PROTACs) targeting METTL3 and identified KH12 as a potent METTL3 degrader. Treatment of KH12 on MOLM-13 cells causes more than 80% degradation of METTL3 with a half-maximal degradation concentration (DC50) of 220 nM in a dose-, time- and ubiquitin-dependent fashion. In addition… Show more
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