Inhibition of the interleukin-1 beta converting enzyme family rescues neurons from apoptotic death

Mol Psychiatry. 1997 May;2(3):227-38. doi: 10.1038/sj.mp.4000242.

Abstract

The interleukin-1 beta converting enzyme (ICE) family of cysteine proteases has been implicated in apoptosis. This study tested the effects of a novel pan-ICE family inhibitor, bocaspartyl(OMe)-fluoromethylketone (boc-Asp-CH2F), against low potassium-induced apoptosis of cultured rat cerebellar granule neurons (CGN). A single application of this cell-permeant compound (20 microM) inhibited apoptotic cell death up to 48 h. Classical apoptotic changes were monitored by fluorescence microscopy, DNA fragmentation and scanning electron microscopy (SEM). A control peptidic fluoromethylketone (boc-Thr-CH2F), and inhibitors to calpain (Ac-Leu-Leu-norleucinal), cathepsin B (Z-Phe-Ala-CH2F), and CPP32-like proteases (Z-DEVD-CH2F), failed to prevent apoptotic death. An 35S-methionine incorporation assay verified that, unlike cycloheximide, boc-Asp-CH2F did not inhibit protein synthesis, hence excluding this as a rescuing mechanism. Although ICE was not detected by northern blot analysis, both CPP32 and Nedd2 expression were found to increase during apoptosis. Kinetic assays with cell extracts from boc-Asp-CH2F-treated neurons measured reduced rates of cleavage for DEVD-pNA and LEVD-pNA. At present, ICE-like proteases remain viable candidates for mediating neuronal death.

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Aspartic Acid / analogs & derivatives*
  • Aspartic Acid / pharmacology
  • Caspase 1
  • Cells, Cultured
  • Cysteine Endopeptidases / drug effects*
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology*
  • Neurons / drug effects*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Enzyme Inhibitors
  • benzyloxycarbonyl-aspartyl-fluoromethane
  • Aspartic Acid
  • Cysteine Endopeptidases
  • Caspase 1