Exploiting the selectivity of protein phosphatase 1 for pharmacological intervention

FEBS J. 2013 Jan;280(2):766-70. doi: 10.1111/j.1742-4658.2012.08535.x. Epub 2012 Mar 14.

Abstract

Selective and reversible phosphorylation is one of the most common post-translational modifications of proteins. Although kinase inhibitors are popular in drug development programmes, selective pharmacological manipulation of phosphatase activity has been challenging to achieve. We review recent advances in the development of selective inhibitors of dephosphorylation events and discuss the potential applications of small-molecule phosphatase inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Enzyme Inhibitors / pharmacology*
  • Eukaryotic Initiation Factor-2 / metabolism
  • Guanabenz / pharmacology
  • Humans
  • Models, Biological
  • Phosphorylation / drug effects
  • Protein Phosphatase 1 / antagonists & inhibitors*
  • Protein Phosphatase 1 / metabolism*
  • Signal Transduction / drug effects*

Substances

  • Enzyme Inhibitors
  • Eukaryotic Initiation Factor-2
  • PPP1R15A protein, human
  • Protein Phosphatase 1
  • Guanabenz