Restoring functions of tumor suppressors with small molecules.

Abstract 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 .