Protein Phosphatases: A Neglected Target Family for Drug Discovery

The gene family of protein phosphatases is a rich but under-exploited source therapeutically validated drug targets modulating signal transduction pathways. Unlike the kinase family, research and development activities have not yet yielded any approved small-molecule drugs against phosphatase. Approximately 20 years ago, phosphatase was classified as undruggable intractable. This primarily due to spectacular failure cumulated industry-wide discovery efforts develop PTP1B inhibitors. Recently, allosteric inhibitors SHP2, member entered clinical trails, which has reawakened industry’s interest towards this neglected enzyme family. contribution reviews recent R&D trends around modulators over last years, rather than providing an exhaustive review field