Mass Spectrometry Investigation of the Binding Sites of a Small-Molecule STAT3-STAT3 Inhibitor

摘要

Stattic was one of the first molecules to be identified as a specific inhibitor of STAT3 phosphorylation, dimerization and function. Through this study, we have shown for the first time that Stattic molecules binds to cysteine residues in a non-specific manner, with up to 5 binding sites identified using LC-MS/MS. These results may be used as a basis for the rational design of novel inhibitors that target key Cys residues to inhibit STAT3 function.