Cellular pharmacology of protein kinase Mζ (PKMζ) contrasts with its in vitro profile: implications for PKMζ as a mediator of memory

J Biol Chem. 2012 Apr 13;287(16):12879-85. doi: 10.1074/jbc.M112.357244. Epub 2012 Feb 29.

Abstract

A number of recent studies have used pharmacological inhibitors to establish a role for protein kinase Mζ (PKMζ) in synaptic plasticity and memory. These studies use zeta inhibitory peptide (ZIP) and chelerythrine as inhibitors of PKMζ to block long term potentiation and memory; staurosporine is used as a negative control to show that a nonspecific kinase inhibitor does not block long term potentiation and memory. Here, we show that neither ZIP nor chelerythrine inhibits PKMζ in cultured cells or brain slices. In contrast, staurosporine does block PKMζ activity in cells and brain slices by inhibiting its upstream phosphoinositide-dependent kinase-1. These studies demonstrate that the effectiveness of drugs against purified PKMζ may not be indicative of their specificity in the more complex environment of the cell and suggest that PKMζ is unlikely to be the mediator of synaptic plasticity or memory.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Benzophenanthridines / pharmacology
  • COS Cells
  • Chlorocebus aethiops
  • Enzyme Inhibitors / pharmacology
  • HEK293 Cells
  • HeLa Cells
  • Hippocampus / drug effects*
  • Hippocampus / enzymology*
  • Humans
  • Memory / physiology*
  • Neuronal Plasticity / physiology
  • Organ Culture Techniques
  • Peptides / pharmacology
  • Phosphorylation / drug effects
  • Phosphorylation / physiology
  • Protein Kinase C / antagonists & inhibitors
  • Protein Kinase C / metabolism*
  • Rats
  • Staurosporine / pharmacology

Substances

  • Antineoplastic Agents
  • Benzophenanthridines
  • Enzyme Inhibitors
  • Peptides
  • chelerythrine
  • Protein Kinase C
  • protein kinase M zeta, rat
  • Staurosporine