Table 2.
Inhibitors and mechanisms of FTO discovered to date.
| Inhibitors' name | Experimental subject (in vivo/in vitro) | Mechanisms of inhibitors | References |
|---|---|---|---|
| Rhein | BE (2)-C cells | Competitively binds to the FTO active site in vitro | Chen et al., 2012 |
| Meclofenamic acid | HeLa cells | Competes with FTO on m6A-containing substrate binding over ALKBH5 | Huang et al., 2015 |
| N-CDPCB, 1a | 3T3-L1 cells | An antiparallel β-sheet and the L1 loop of FTO sandwich N-CDPCB | He et al., 2015 |
| CHTB | 3T3-L1 cells | CHTB can bind to the FTO active site | Qiao et al., 2016 |
| Entacapone | DIO mice/Hep-G2 cells | Directly bound to FTO and inhibited FTO activity in vitro | Peng et al., 2019 |
| Radicicol | —— | Adopts an L-shaped conformation in the FTO binding site and occupies the same position as N-CDPCB | Wang et al., 2018 |
CHTB, 4-chloro-6-(6′-chloro-7′-hydroxy-2′,4′,4′-trimethyl-chroman-2′-yl)benzene-1,3-diol; DIO, diet-induced obese; FTO, fat mass and obesity associated protein; N-CDPCB, 1a, N-(5-Chloro-2,4-dihydroxyphenyl)-1-phenylcyclobutanecarboxamide; “——” indicates that there are no corresponding animals and cells used in the literature we cited.