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Molecular Insights to the Bioactive Form of BV02, a Reference Inhibitor of 14-3-3σ Protein-Protein Interactions

Molecular Insights to the Bioactive Form of BV02, a Reference Inhibitor of 14-3-3σ Protein-Protein Interactions

Daniela Valensin, Ylenia Cau, Pierpaolo Calandro, Giulia Vignaroli, Lucia Dello Iacono, Mario Chiariello, Mattia Mori, Maurizio Botta

Bioorg Med Chem Lett. 2016 Feb 1;26(3):894-898.

PMID: 26774582

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP292870532	BV02		292870-53-2	Price

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