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 / Stornaiuolo, M.; LA REGINA, Giuseppe; Passacantilli, Sara; Grassia, G.; Coluccia, Antonio; La Pietra, V.; Giustiniano, M.; Cassese, H.; Di Maro, S.; Brancaccio, D.; Taliani, S.; Ialenti, A.; Silvestri, Romano; Martini, C.; Novellino, E.; Marinelli, L.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 58:5(2015), pp. 2135-2148. [10.1021/jm501123r]

Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents

LA REGINA, GIUSEPPE;PASSACANTILLI, SARA;COLUCCIA, Antonio;SILVESTRI, Romano;
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.
2015
lewis lung-carcinoma; proapoptotic bax; cell-line; inhibitors; apoptosis; therapy; docking; glide
01 Pubblicazione su rivista::01a Articolo in rivista
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents / Stornaiuolo, M.; LA REGINA, Giuseppe; Passacantilli, Sara; Grassia, G.; Coluccia, Antonio; La Pietra, V.; Giustiniano, M.; Cassese, H.; Di Maro, S.; Brancaccio, D.; Taliani, S.; Ialenti, A.; Silvestri, Romano; Martini, C.; Novellino, E.; Marinelli, L.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 58:5(2015), pp. 2135-2148. [10.1021/jm501123r]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/764095
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