Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

S-phase kinase-associated protein 2 (SKP2)

In vitro, cell culture and mouse studies identified SKP2 inhibitors that could be useful for treating cancer. An in silico screen and in vitro assays identified a small molecule, 3-(1,3-benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, that blocked the interaction between SKP1 and SKP2 at low micromolar concentrations and specifically inhibited the ubiquitination of SKP2 substrates. In cancer cell lines, the compound decreased growth and the expression of cancer stem cell surface markers compared with vehicle. In mouse xenograft models of lung or prostate cancer, the compound also decreased tumor growth. Next steps include lead optimization.

SciBX 6(34); doi:10.1038/scibx.2013.923
Published online Sept. 5, 2013

Patent application filed; available for licensing

Chan, C.-H. et al. Cell;
published online Aug. 1, 2013;
doi:10.1016/j.cell.2013.06.048
Contact: Hui-Kuan Lin,
The University of Texas MD Anderson Cancer Center, Houston, Texas
e-mail:
hklin@mdanderson.org
Contact: Shuxing Zhang,
 same affiliation as above
e-mail:
shuzhang@mdanderson.org