A yeast-based model of alpha-synucleinopathy identifies compounds with therapeutic potential

Biochim Biophys Acta. 2006 Mar;1762(3):312-8. doi: 10.1016/j.bbadis.2005.11.009. Epub 2005 Dec 27.

Abstract

We have developed a yeast-based model recapitulating neurotoxicity of alpha-synuclein fibrilization. This model recognized metal ions, known risk factors of alpha-synucleinopathy, as stimulators of alpha-synuclein aggregation and cytotoxicity. Elimination of Yca1 caspase activity augmented both cytotoxicity and inclusion body formation, suggesting the involvement of apoptotic pathway components in toxic alpha-synuclein amyloidogenesis. Deletion of hydrophobic amino acids at positions 66-74 in alpha-synuclein reduced its cytotoxicity but, remarkably, did not lower the levels of insoluble alpha-synuclein, indicating that noxious alpha-synuclein species are different from insoluble aggregates. A compound screen aimed at finding molecules with therapeutic potential identified flavonoids with strong activity to restrain alpha-synuclein toxicity. Subsequent structure-activity analysis elucidated that these acted by virtue of anti-oxidant and metal-chelating activities. In conclusion, this yeast-cell model as presented allows not only fundamental studies related to mechanisms of alpha-synuclein-instigated cellular degeneration, but is also a valid high-throughput identification tool for novel neuroprotective agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Brain Diseases / drug therapy*
  • Brain Diseases / metabolism
  • Brain Diseases / pathology*
  • Caspase Inhibitors
  • Caspases / metabolism
  • Catechin / analogs & derivatives
  • Catechin / chemistry
  • Catechin / metabolism
  • Catechin / therapeutic use
  • Flavonoids / chemistry
  • Flavonoids / metabolism
  • Flavonoids / therapeutic use
  • Humans
  • Metals / metabolism
  • Models, Biological*
  • Molecular Structure
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / metabolism
  • Neuroprotective Agents / therapeutic use
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Risk Factors
  • Saccharomyces cerevisiae / chemistry
  • Saccharomyces cerevisiae / genetics
  • Saccharomyces cerevisiae / metabolism*
  • Saccharomyces cerevisiae Proteins / antagonists & inhibitors
  • Saccharomyces cerevisiae Proteins / metabolism
  • alpha-Synuclein / chemistry
  • alpha-Synuclein / genetics
  • alpha-Synuclein / metabolism*
  • alpha-Synuclein / toxicity

Substances

  • Caspase Inhibitors
  • Flavonoids
  • Metals
  • Neuroprotective Agents
  • Recombinant Fusion Proteins
  • Saccharomyces cerevisiae Proteins
  • alpha-Synuclein
  • Catechin
  • epigallocatechin gallate
  • Caspases
  • MCA1 protein, S cerevisiae