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

• DOI: 10.1002/jmr.2800
• Publication Date: 2019-07-19T08:42:07Z
• Authors: Ying Wang; Junya Li; Xinxin Han; Ning Wang; Chuanjun Song; Ruiyong Wang; Junbiao Chang
• Keywords: Demethylase; Anti obesity; Carbazole

Abstract The alkaloids containing a carbazole nucleus are an established class of natural products with wide range biological activities. A combination thermodynamic and enzymatic activity studies provides insight into the recognition Clausine E by fat mass obesity‐associated protein (FTO). binding to FTO was driven positive entropy negative enthalpy changes. Results also indicated that hydroxyl group crucial for small molecules FTO. structural information basis design more effective inhibitors demethylase activity.