Home
Resources
Publications
Chemically Stable Inhibitors of 14-3-3 Protein-Protein Interactions Derived From BV02

Chemically Stable Inhibitors of 14-3-3 Protein-Protein Interactions Derived From BV02

Leire Iralde-Lorente, Ylenia Cau, Letizia Clementi, Lorenzo Franci, Giusy Tassone, Daniela Valensin, Mattia Mori, Adriano Angelucci, Mario Chiariello, Maurizio Botta

J Enzyme Inhib Med Chem. 2019 Dec;34(1):657-664.

PMID: 30727786

Abstract:

14-3-3 are regulatory proteins that through protein-protein interactions (PPI) with numerous binding partners could be involved in several human diseases, including cancer, neurodegenerative disorders, and pathogens infections. Following our research interest in the development of 14-3-3 PPI inhibitors, here we exploited the privileged 4-aminoantipyrine scaffold in the design and synthesis of some derivatives endowed with antiproliferative activity against K-562 cells, and capable of binding to recombinant 14-3-3σ as evidenced by NMR spectroscopy. The binding mode was further explored by molecular modelling, while coupling confocal microscopy with intensitometric analysis showed that compound 1 was able to promote the nuclear translocation of c-Abl at low micromolar concentrations. Overall, 1 is chemically stable compared to parent 14-3-3 PPI inhibitors, and thus emerged as a confirmed hit for further development.

Chemicals Related in the Paper:

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

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: