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Updated: Mar 27, 2026

Bio-layer Interferometry for Measuring Kinetics of Protein-protein Interactions and Allosteric Ligand Effects
Published on: February 18, 2014
Molecular insights to the bioactive form of BV02, a reference inhibitor of 14-3-3σ protein-protein interactions
Daniela Valensin1, Ylenia Cau1, Pierpaolo Calandro1
1Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli studi di Siena, via A. Moro snc, Via Aldo Moro 2, 53100 Siena, Italy.
Abstract:
BV02 is a reference inhibitor of 14-3-3 protein-protein interactions, which is currently used as chemical biology tool to understand the role of 14-3-3 proteins in pathological contexts. Due to chemical instability in certain conditions, its bioactive form has remained unclear. Here, we use NMR spectroscopy to prove for the first time the direct interaction between the molecule and 14-3-3σ, and to depict its bioactive form, namely the phthalimide derivative 9. Our work provides molecular insights to the bioactive form of the 14-3-3 PPI inhibitor and facilitates further development as candidate therapeutic agent.
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