Protein Phosphatases: A Neglected Target Family for Drug Discovery


  • Joe Lewis Anavo Therapeutics, Heidelberg
  • Gerhard Müller Anavo Therapeutics, J.H. Oortweg 19, 233 CH Leiden, NL



Allosteric inhibitors, Inhibitors, Kinases, Phosphatases, PTP1B, SHP2, Target family


The gene family of protein phosphatases is a rich but under-exploited source of 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 a phosphatase. Approximately 20 years ago, the phosphatase family was classified as undruggable and intractable. This was primarily due to the spectacular failure of the cumulated industry-wide drug discovery efforts to develop PTP1B inhibitors. Recently, allosteric inhibitors against SHP2, a member of the phosphatase family, have entered clinical trails, which has reawakened industry’s interest towards this neglected enzyme family. This contribution reviews the recent R&D trends around small-molecule efforts towards phosphatase modulators over the last years, rather than providing an exhaustive review of the field of allosteric phosphatase inhibitors.




How to Cite

J. Lewis, G. Müller, Chimia 2022, 76, 460, DOI: 10.2533/chimia.2022.460.



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