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.

Structure-Based Lead Optimization and Biological Evaluation of BAX Direct Activators as Novel Potential Anticancer Agents.

TALIANI, SABRINA;MARTINI, CLAUDIA;
2015

Abstract

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.
Stornaiuolo, M; La Regina, G; Passacantilli, S; Grassia, G; Coluccia, A; La Pietra, V; Giustiniano, M; Cassese, H; Di Maro, S; Brancaccio, D; Taliani, Sabrina; Ialenti, A; Silvestri, R; Martini, Claudia; Novellino, E; Marinelli, L.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/744873
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