Structure-Based Lead Optimization and Biological Evaluation of BAX Direct Activators as Novel Potential Anticancer Agents
Year: 2015
Type: article
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.
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm501123r
Authors: Mariano Stornaiuolo, Giuseppe La Regina, Sara Passacantilli, Gianluca Grassia, Antonio Coluccia, Valeria La Pietra, Mariateresa Giustiniano, Hilde Cassese, Salvatore Di Maro, Diego Brancaccio, Sabrina Taliani, Armando Ialenti, Romano Silvestri, Claudia Martini, Ettore Novellino, Luciana Marinelli
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2328035482