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

中文翻译：

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将Clausine E鉴定为脂肪量和肥胖相关蛋白（FTO）脱甲基酶活性的抑制剂。

含有咔唑核的生物碱是一类已确立的具有广泛生物活性的天然产物。热力学和酶活性研究的结合提供了对脂肪量和肥胖相关蛋白（FTO）对克劳斯丁E识别的认识。Clausine E与FTO的结合是由正熵和负焓变化驱动的。结果还表明，羟基对于小分子与FTO的结合至关重要。结构和热力学信息为设计更有效的FTO脱甲基酶活性抑制剂提供了基础。