Journal
CHEMICO-BIOLOGICAL INTERACTIONS
Volume 297, Issue -, Pages 80-84Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2018.10.023
Keywords
Fat mass and obesity-associated protein; Nafamostat mesilate; Inhibitor
Funding
- National Natural Science Foundation of China [81330075]
- Key science and technology plan project of Henan province [152102310065]
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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.
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