Identification of presenilin 1-selective γ-secretase inhibitors with reconstituted γ-secretase complexes.

  title={Identification of presenilin 1-selective γ-secretase inhibitors with reconstituted γ-secretase complexes.},
  author={Julie M. Lee and L. Song and G. Terracina and Thomas A. Bara and H. Josien and T. Asberom and T. Sasikumar and D. Burnett and J. Clader and E. Parker and L. Zhang},
  volume={50 22},
  • Julie M. Lee, L. Song, +8 authors L. Zhang
  • Published 2011
  • Biology, Medicine
  • Biochemistry
  • Accumulation of the β-amyloid (Aβ) peptides is one of the major pathologic hallmarks in the brains of Alzheimer's disease (AD) patients. Aβ is generated by sequential proteolytic cleavage of the amyloid precursor protein (APP) catalyzed by β- and γ-secretases. Inhibition of Aβ production by γ-secretase inhibitors (GSIs) is thus being pursued as a target for treatment of AD. In addition to processing APP, γ-secretase also catalyzes proteolytic cleavage of other transmembrane substrates, with the… CONTINUE READING
    27 Citations
    γ-Secretase inhibitors and modulators.
    • 179
    Complex regulation of γ-secretase: from obligatory to modulatory subunits
    • 29
    • PDF
    Presenilin 1 and Presenilin 2 Target γ-Secretase Complexes to Distinct Cellular Compartments*
    • 31
    • PDF
    Evidence that Enzyme Processivity Mediates Differential Aβ Production by PS1 and PS2
    • 6
    • PDF
    Alzheimer's Disease: Presenilin 2-Sparing γ-Secretase Inhibition Is a Tolerable Aβ Peptide-Lowering Strategy
    • 35
    • PDF
    The development of an in vivo γ-secretase assay using zebrafish embryos.
    • 9


    Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors*
    • 271
    • PDF
    Identification of γ-Secretase Inhibitor Potency Determinants on Presenilin*
    • 50
    • PDF
    Reconstitution of γ-secretase activity
    • 765
    gamma-Secretase in biology and medicine.
    • M. Wolfe
    • Biology, Medicine
    • Seminars in cell & developmental biology
    • 2009
    • 75