Endo Y, Hashimoto Y, Fukasawa H, Shudo K
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Biochem Biophys Res Commun. 1993 Aug 16;194(3):1529-35. doi: 10.1006/bbrc.1993.1998.
Several oxygenated cholesterols and their derivatives (yakkasteroids) were prepared as candidate ligands for cytosolic-nuclear tumor promoter binding protein (CN-TPBP). Among the compounds, a possible natural substance, 3 beta,5 alpha-dihydroxycholestan-6-one (yakkasterone), showed the highest binding affinity to CN-TPBP. It also showed high specificity for binding to CN-TPBP: it does not bind to protein kinase C. Investigation of the structure-activity relationships of yakkasteroids revealed that the structure of the side chain at the 20-position is important for the binding activity to CN-TPBP.
