Small Molecule Inhibitors of Serine Threonine Protein Phosphatases

Authors: McCluskey A.; Sakoff J.A.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 1, May 2001 , pp. 43-55(13)

Publisher: Bentham Science Publishers

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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