The functional gamma-secretase inhibitor prevents production of amyloid beta 1-34 in human and murine cell lines

Neurosci Lett. 2001 Nov 27;315(3):145-8. doi: 10.1016/s0304-3940(01)02369-2.

Abstract

The amyloid precursor protein (APP) undergoes two consecutive cleavages by different proteases, beta-secretase and gamma-secretase, leading to the release of an amyloidogenic 4 kDa fragment called amyloid beta (Abeta). Combining immunoprecipitation and mass spectrometry, we characterized soluble Abeta in cultured cell media of mouse neuroblastoma N2a cells and double hAPP/hBACE-1 transfected HEK293. The major Abeta isoforms detected were Abeta11-34, Abeta1-34, Abeta11-40 and Abeta1-40. In this study, we demonstrate that overexpression of human beta-secretase (BACE-1) in HEK293 cells resulted in predominant Abeta cleavage at position Glu(11) rather than Asp(1), as well as increased production of Abeta(x)-34, but not Abeta(x)-40. Incubation of cells with a specific gamma-secretase inhibitor suggests that cleavage of APP at Leu(34) could be mediated by gamma-secretase itself or by a gamma-secretase dependent process.

MeSH terms

  • Amyloid Precursor Protein Secretases
  • Amyloid beta-Peptides / analysis
  • Amyloid beta-Peptides / antagonists & inhibitors
  • Amyloid beta-Peptides / biosynthesis*
  • Amyloid beta-Peptides / chemistry
  • Amyloid beta-Protein Precursor / chemistry
  • Amyloid beta-Protein Precursor / genetics
  • Amyloid beta-Protein Precursor / metabolism
  • Animals
  • Aspartic Acid Endopeptidases / genetics
  • Aspartic Acid Endopeptidases / pharmacology
  • Cell Line
  • Culture Media / chemistry
  • Endopeptidases / drug effects
  • Endopeptidases / physiology*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Mice
  • Peptide Fragments / analysis
  • Peptide Fragments / antagonists & inhibitors
  • Peptide Fragments / biosynthesis*
  • Protein Isoforms / analysis
  • Solubility
  • Transfection

Substances

  • Amyloid beta-Peptides
  • Amyloid beta-Protein Precursor
  • Culture Media
  • Enzyme Inhibitors
  • Peptide Fragments
  • Protein Isoforms
  • amyloid beta-protein (1-34)
  • Amyloid Precursor Protein Secretases
  • Endopeptidases
  • Aspartic Acid Endopeptidases
  • BACE1 protein, human
  • Bace1 protein, mouse