Affiliation: Drug Discovery Institute, Biomedical Science Tower 3, Suite 10040, 3501 Fifth Avenue, University of Pittsburgh, Pittsburgh, PA 15260, USA.
Proper control of cell cycle progression requires the functionality of a small family of activating phosphatases termed Cdc25, which have been implicated in cancer and Alzheimers disease. These protein tyrosine phosphatases are therefore recognized as attractive molecular targets for small molecules. We review the rationale, approaches, progress and challenges for developing small molecule inhibitors of the Cdc25 family. A number of potential chemical probes are discussed and their characteristics are summarized.