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Vasolin containing protein (VCP; p97)

In vitro studies identified two new classes of VCP inhibitors that could help treat cancer. High throughput screening of a small molecule library and in vitro testing identified two hits. One inhibited VCP via covalent binding of its ATPase site and the other by noncovalent binding of an allosteric site. Optimization of the allosteric site-binding hit yielded a lead compound that bound VCP and inhibited growth of multiple human cancer cell lines at nanomolar to low micromolar IC50 values. Future work by Nerviano Medical Sciences s.r.l. and its collaborator, the Genentech Inc. unit of Roche, could include testing the lead allosteric inhibitor in animal models of cancer.
Cleave Biosciences Inc. has a discovery-stage VCP inhibitor program to treat cancer.

SciBX 6(32); doi:10.1038/scibx.2013.859
Published online Aug. 22, 2013

Patent and licensing status undisclosed

Magnaghi, P. et al. Nat. Chem. Biol.; published online July 28, 2013;
Contact: Paola Magnaghi, Nerviano Medical Sciences s.r.l., Nerviano, Italy