Mini-Reviews in Medicinal Chemistry

Author(s): Adam McCluskey and Jennette A. Sakoff

DOI: 10.2174/1389557013407205

Small Molecule Inhibitors of Serine Threonine Protein Phosphatases

Page: [43 - 55] Pages: 13

  • * (Excluding Mailing and Handling)

Abstract

Serine(slash)threonine protein phosphatases have long been ignored as potential therapeutic targets for two reasons, one the biochemical significance of these proteins has not been appreciated and two, many natural protein phosphatase inhibitors are potent toxins and are considered unsuitable for clinical use. This review outlines the biochemical role of this protein family in cancer, cystic fibrosis, immunosuppression and, cardiac and neurological disorders. Particular emphasis is also given to the synthesis of selective small molecule inhibitors and their clinical

Keywords: Molecule Inhibitors, Protein Phosphatases, phosphorylation, C terminal, PP1 and PP2A, Gene mutations, myopathic disease, okadaic acid, cantharidin analogues, family of Coleoptera, alfalfahay