Exploiting the selectivity of protein phosphatase 1 for pharmacological intervention


A. Bertolotti, MRC Laboratory of Molecular Biology, Hills Road, Cambridge CB2 0QH, UK
Fax: +44 (0)1223 402310
Tel: +44 (0)1223 402203
E-mail: aberto@mrc-lmb.cam.ac.uk


Selective and reversible phosphorylation is one of the most common post-translational modifications of proteins. Although kinase inhibitors are popular in drug development programmes, selective pharmacological manipulation of phosphatase activity has been challenging to achieve. We review recent advances in the development of selective inhibitors of dephosphorylation events and discuss the potential applications of small-molecule phosphatase inhibitors.