Restoring functions of tumor suppressors with small molecules.

Developing small molecule inhibitors of oncoproteins, which are activated in tumor cells, is a newly popular strategy for cancer-related drug discovery. The complementary strategy, developing small molecules that restore the function of missing tumor suppressors, is much more difficult to realize. However, in this issue of Cancer Cell, Kau et al. report the discovery of small molecules that reverse some cellular consequences of the loss of the tumor suppressor PTEN.