Investigation of the interaction between FTO and 3-substituted 2-aminochromones by spectroscopy and molecular modeling

Identification of Clausine E as an inhibitor of fat mass and obesity‐associated protein (FTO) demethylase activity

“…The ITC result indicated that Clausine E can bind to FTO protein and the biochemical assay showed that Clausine E displays inhibitory activity of demethylation of the ssRNA by FTO. On the basis of our previous results, if the interaction between FTO and Clausine E occurred, the fluorescence intensity of FTO protein would be quenched by Clausine E.…”

“…Our previous work shows that the intrinsic fluorescence of FTO can be quenched by 1,3‐diazaheterocyclic compounds, 3‐substituted 2‐aminochromones, camptothecin, flavonols, clenbuterol, and so on. The interactions of FTO with various small molecules revealed that the interaction forces were mainly determined by the structures of small molecules.…”

“…The intensity decreased regularly with the addition of Clausine E, which indicates that Clausine E may interact with FTO. In order to examine the fluorescence quenching mechanism, the well‐known Stern‐Volmer equation was used as described in previous publications …”

“…Continuing our work on the development of new inhibitors of FTO, we herein report the interactions between FTO protein and a series of carbazole alkaloids. We screen potential FTO inhibitors using isothermal titration calorimetry (ITC), liquid chromatography‐mass spectrometry (LC‐MS), and spectral approaches and report structural and thermodynamic studies of the interaction between Clausine E and FTO for the first time.…”

The role of chlorine atom on the binding between 2‐phenyl‐1H‐benzimidazole analogues and fat mass and obesity‐associated protein

“…Our previous work showed that the fluorescence intensity of FTO will be quenched if the interactions occurred between FTO and small molecules . In this work, we investigated the influence of 1d on the fluorescence spectra of FTO as shown in Figure .…”