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858 Therapeutics is developing a preclinical small molecule inhibitor targeting METTL3 (methyltransferase-like 3) for the treatment of solid tumors. METTL3 is the catalytic subunit of the m6A methyltransferase complex, which installs N6-methyladenosine (m6A) modifications on mRNA. This epigenetic modification is a key regulator of RNA stability, splicing, and translation. In various cancers, METTL3 is overexpressed, leading to the dysregulation of oncogenic transcripts that drive tumor proliferation and survival. By inhibiting METTL3's catalytic activity, the program aims to disrupt these oncogenic pathways and provide a novel therapeutic approach for solid tumors. This program was acquired by 858 Therapeutics through its acquisition of Gotham Therapeutics in 2021.
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