Stornaiuolo Mariano, La Regina Giuseppe, Passacantilli Sara, Grassia Gianluca, Coluccia Antonio, La Pietra Valeria, Giustiniano Mariateresa, Cassese Hilde, Di Maro Salvatore, Brancaccio Diego, Taliani Sabrina, Ialenti Armando, Silvestri Romano, Martini Claudia, Novellino Ettore, Marinelli Luciana
Dipartimento di Farmacia, Università di Napoli "Federico II" , via D. Montesano 49, 80131 Naples, Italy.
J Med Chem. 2015 Mar 12;58(5):2135-48. doi: 10.1021/jm501123r. Epub 2015 Feb 25.
The first direct activator of BAX, a pro-apoptotic member of the BCL-2 family, has been recently identified. Herein, a structure-based lead optimization turned out into a small series of analogues, where 8 is the most potent compound published so far. 8 was used as pharmacological tool to ascertain, for the first time, the anticancer potential of BAX direct activators and the obtained results would suggest that BAX direct activators are potential future anticancer drugs rather than venoms.
最近发现了BCL-2家族促凋亡成员BAX的首个直接激活剂。在此，基于结构的先导物优化产生了一小系列类似物，其中化合物8是迄今报道的活性最强的化合物。化合物8被用作药理学工具，首次确定BAX直接激活剂的抗癌潜力，所得结果表明BAX直接激活剂是未来潜在的抗癌药物，而非毒液。
