Nur77 (also called TR3) is an orphan nuclear receptor, and plays important roles in carcinogenesis,inflammation, metabolism, and energy homeostasis.There is no physiological ligand identified up to date.Nur77 is of multiple functions in addition to being a transcription factor.These non-transcription functions can be modulated by a variety of small molecules that are distinct to physiological ligands that regulate the ligand-dependent nuclear receptors.In 2008, we identified a natural productfrom an endophytic fungus Dotiorella sp.HTF3,cytosporone B (Csn-B) , as an agonist to activate the transcriptional activity of Nur77 (Zhan et al., Nat Chemical Biology, 2008).Based on Csn-B, a library of Nur77 interacting compounds wasgenerated through synthesis, which sets the basis for in-depth investigations on Nur77 multi-functionality in anti-cancer,-diabetes,-inflammation, and so on.