Neuroprotection by pharmacologic blockade of the GAPDH death cascade

Proc Natl Acad Sci U S A. 2006 Mar 7;103(10):3887-9. doi: 10.1073/pnas.0511321103. Epub 2006 Feb 27.

Abstract

Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) participates in a cell death cascade wherein a variety of stimuli activate nitric oxide (NO) synthases with NO nitrosylating GAPDH, conferring on it the ability to bind to Siah, an E3-ubiquitin-ligase, whose nuclear localization signal enables the GAPDH/Siah protein complex to translocate to the nucleus where degradation of Siah targets elicits cell death. R-(-)-Deprenyl (deprenyl) ameliorates the progression of disability in early Parkinson's disease and also has neuroprotective actions. We show that deprenyl and a related agent, TCH346, in subnanomolar concentrations, prevent S-nitrosylation of GAPDH, the binding of GAPDH to Siah, and nuclear translocation of GAPDH. In mice treated with the dopamine neuronal toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), low doses of deprenyl prevent binding of GAPDH and Siah1 in the dopamine-enriched corpus striatum.

Publication types

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

MeSH terms

  • Animals
  • Antiparkinson Agents / pharmacology
  • Apoptosis / drug effects*
  • Apoptosis / physiology
  • Cell Line
  • Glyceraldehyde-3-Phosphate Dehydrogenases / antagonists & inhibitors*
  • Glyceraldehyde-3-Phosphate Dehydrogenases / physiology
  • Humans
  • In Vitro Techniques
  • MPTP Poisoning / pathology
  • MPTP Poisoning / physiopathology
  • Male
  • Mice
  • Nerve Degeneration / pathology
  • Nerve Degeneration / physiopathology
  • Nerve Degeneration / prevention & control
  • Neuroprotective Agents / pharmacology*
  • Nitric Oxide / metabolism
  • Nuclear Proteins / physiology
  • Oxepins / pharmacology
  • Parkinson Disease / drug therapy
  • Selegiline / pharmacology
  • Ubiquitin-Protein Ligases / physiology

Substances

  • Antiparkinson Agents
  • Neuroprotective Agents
  • Nuclear Proteins
  • Oxepins
  • dibenzo(b,f)oxepin-10-ylmethyl-methyl-prop-2-ynyl-amine
  • Selegiline
  • Nitric Oxide
  • Glyceraldehyde-3-Phosphate Dehydrogenases
  • Ubiquitin-Protein Ligases
  • seven in absentia proteins