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

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.

doi:10.1021/jm501123r

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.

Autori interni:	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. mostra contributor esterni nascondi contributor esterni
Autori:	Stornaiuolo M;La Regina G;Passacantilli S;Grassia G;Coluccia A;La Pietra V;Giustiniano M;Cassese H;Di Maro S;Brancaccio D;Taliani S;Ialenti A;Silvestri R;Martini C;Novellino E;Marinelli L
Titolo:	Structure-Based Lead Optimization and Biological Evaluation of BAX Direct Activators as Novel Potential Anticancer Agents.
Anno del prodotto:	2015
Digital Object Identifier (DOI):	10.1021/jm501123r
Appare nelle tipologie:	1.1 Articolo in rivista

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