MINIREVIEW Targeting Protein Serine/Threonine Phosphatases for Drug Development

With the recent clinical success of drugs targeting protein ki-nase activity, drug discovery efforts are focusing on the role of reversible protein phosphorylation in disease states. The activ-ity of protein phosphatases, enzymes that oppose protein ki-nases, can also be manipulated to alter cellular signaling for therapeutic benefits. In this review, we present protein serine/ threonine phosphatases as viable therapeutic targets, discuss-ing past successes, current challenges, and future strategies for modulating phosphatase activity. Numerous cellular processes, including metabolism, im-mune response, synaptic plasticity, cell growth and prolifer-ation, and apoptosis, are controlled by intricate signal trans-duction networks composed of molecules and macromolecular protein complexes that are responsive to biological or chem