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FTO inhibitors target the fat mass and obesity-associated protein (FTO), an RNA demethylase. FTO belongs to the iron- and 2-oxoglutarate-dependent dioxygenases, a family that also removes methyl groups from DNA. In 2007, a common variant in the FTO gene was associated with body mass index and obesity. In 2011, N6-methyladenosine (m6A) in nuclear RNA was identified as a major FTO substrate, the first evidence of reversible RNA methylation. FTO inhibitors are used to study how m6A removal affects messenger RNA (mRNA) stability, adipogenesis and the growth of leukemia and glioblastoma cells. Representative inhibitors listed here include FB23, Dac590, MO-I-500 and FTO-IN-8. The m6A writer and readers are covered by the neighboring categories METTL3 and YTHDF.
