In vitro gamma-secretase cleavage of the Alzheimer's amyloid precursor protein correlates to a subset of presenilin complexes and is inhibited by zinc

FEBS J. 2005 Nov;272(21):5544-57. doi: 10.1111/j.1742-4658.2005.04950.x.

Abstract

The gamma-secretase complex mediates the final proteolytic event in Alzheimer's disease amyloid-beta biogenesis. This membrane complex of presenilin, anterior pharynx defective, nicastrin, and presenilin enhancer-2 cleaves the C-terminal 99-amino acid fragment of the amyloid precursor protein intramembranously at gamma-sites to form C-terminally heterogeneous amyloid-beta and cleaves at an epsilon-site to release the intracellular domain or epsilon-C-terminal fragment. In this work, two novel in vitro gamma-secretase assays are developed to further explore the biochemical characteristics of gamma-secretase activity. During development of a bacterial expression system for a substrate based on the amyloid precursor protein C-terminal 99-amino acid sequence, fragments similar to amyloid-beta and an epsilon-C-terminal fragment were observed. Upon purification this substrate was used in parallel with a transfected source of substrate to measure gamma-secretase activity from detergent extracted membranes. With these systems, it was determined that recovery of size-fractionated cellular and tissue-derived gamma-secretase activity is dependent upon detergent concentration and that activity correlates to a subset of high molecular mass presenilin complexes. We also show that by changing the solvent environment with dimethyl sulfoxide, detection of epsilon-C-terminal fragments can be elevated. Lastly, we show that zinc causes an increase in the apparent molecular mass of an amyloid precursor protein gamma-secretase substrate and inhibits its cleavage. These studies further refine our knowledge of the complexes and biochemical factors needed for gamma-secretase activity and suggest a mechanism by which zinc dysregulation may contribute to Alzheimer's disease pathogenesis.

Publication types

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

MeSH terms

  • Amyloid Precursor Protein Secretases
  • Amyloid beta-Protein Precursor / metabolism*
  • Animals
  • Brain / metabolism
  • COS Cells
  • Cell Membrane / genetics
  • Cell Membrane / metabolism
  • Chlorocebus aethiops
  • Chromatography, Gel
  • Dimethyl Sulfoxide / pharmacology
  • Endopeptidases / genetics
  • Endopeptidases / isolation & purification
  • Endopeptidases / metabolism*
  • Escherichia coli / genetics
  • Escherichia coli / metabolism
  • Gene Expression
  • Guinea Pigs
  • Membrane Proteins / metabolism*
  • Membranes / metabolism
  • Molecular Weight
  • Multiprotein Complexes / metabolism*
  • Protein Binding / drug effects
  • Protein Processing, Post-Translational / drug effects*
  • Substrate Specificity
  • Zinc / pharmacology*

Substances

  • Amyloid beta-Protein Precursor
  • Membrane Proteins
  • Multiprotein Complexes
  • Amyloid Precursor Protein Secretases
  • Endopeptidases
  • Zinc
  • Dimethyl Sulfoxide