Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact
information

Cancer

Cancer

Protein phosphatase magnesium-dependent 1d (PPM1D; WIP1)

In vitro and mouse studies identified an allosteric inhibitor of WIP1 that could help treat cancer. WIP1 is overexpressed in some cancers and dephosphorylates tumor suppressor genes to block their activity. In multiple cancer cell lines expressing WIP1, a WIP1 inhibitor that bound a specific subdomain near the catalytic site increased phosphorylation of p53 and other tumor suppressor genes and decreased cell growth compared with vehicle. In mice with B cell lymphoma xenografts, the allosteric inhibitor decreased tumor growth compared with vehicle. Next steps include optimization of the inhibitor's pharmaceutical properties for clinical evaluation.

SciBX 7(5); doi:10.1038/scibx.2014.140
Published online Feb. 6, 2014

Patent application filed by GlaxoSmithKline plc;
unavailable for licensing

Gilmartin, A.G. et al. Nat. Chem. Biol.; published online Jan. 5, 2014;
doi:10.1038/nchembio.1427
Contact: Rakesh Kumar, GlaxoSmithKline plc, Collegeville, Pa.
e-mail:
rakesh.2.kumar@gsk.com

Contact: Dirk A. Heerding, same affiliation as above
e-mail:
dirk.a.heerding@gsk.com