nsc-36398 and tryptanthrine

Tryptophan 2,3-dioxygenase (TDO) is becoming a promising therapeutic target due to its involvement in cancer and neurodegenerative diseases. Development of efficient TDO inhibitors is a prime strategy in disease treatment. However, the lack of a TDO inhibitor bioassay system slows the progress of TDO inhibitor research. Herein, an active recombinant human TDO (hTDO) was prepared under optimal expression conditions, an enzymatic assay was optimized, and two cellular assays of TDO activity were developed. Then, the potential TDO inhibitory activities of nine tryptanthrin derivatives (5a-5i) were evaluated, and the inhibitory constants (Ki), enzymatic and cellular half maximal inhibitory concentrations (IC

Topics: Dose-Response Relationship, Drug; Enzyme Inhibitors; HEK293 Cells; Humans; Molecular Structure; Quinazolines; Recombinant Proteins; Structure-Activity Relationship; Tryptophan Oxygenase