Nafamostat mesilate is a serine protease inhibitor and used for the treatment of pancreatitis and cancers. The fat mass and obesity-associated protein (FTO) was identified to be a demethylase and played an important role in physiological processes. The aim of this study was to examine the inhibition of Nafamostat mesilate on FTO demethylase activity. A combination of thermodynamic and enzymatic activity studies provides an insight into the recognition of Nafamostat mesilate by FTO. The binding of Nafamostat mesilate to FTO was driven by higher positive entropy changes and smaller negative enthalpy changes. The structural and thermodynamic information provides the basis for the design of more effective inhibitors for FTO. Our results might provide a novel target protein for Nafamostat mesilate.

甲磺酸萘法莫他是一种丝氨酸蛋白酶抑制剂，用于治疗胰腺炎和癌症。脂肪和肥胖相关蛋白（FTO）被确定为脱甲基酶，并且在生理过程中起着重要作用。这项研究的目的是要检查甲磺酸萘法莫他对FTO脱甲基酶活性的抑制作用。热力学和酶活性研究的结合提供了对FTO识别甲磺酸萘法莫他的认识。甲磺酸萘法莫他与FTO的结合是由较高的正熵变化和较小的负焓变化驱动的。结构和热力学信息为设计更有效的FTO抑制剂提供了基础。我们的结果可能为甲磺酸萘法莫他提供了一种新型的靶蛋白。