• Title of article

    Macrocyclic peptidomimetic inhibitors of β-secretase (BACE): First X-ray structure of a macrocyclic peptidomimetic-BACE complex

  • Author/Authors

    Isabel Rojo، نويسنده , , José Alfredo Mart?n، نويسنده , , Howard Broughton، نويسنده , , David Timm، نويسنده , , Jon Erickson، نويسنده , , Hsiu-Chiung Yang، نويسنده , , James R. McCarthy، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2006
  • Pages
    5
  • From page
    191
  • To page
    195
  • Abstract
    The synthesis of novel macrocyclic peptidomimetic inhibitors of the enzyme BACE1 is described. These macrocycles are derived from a hydroxyethylene core structure. Compound 7 was co-crystallized with BACE1 and the X-ray structure of the complex elucidated at 1.6 Å resolution. This molecule inhibits the production of the Aβ peptide in HEK293 cells overexpressing APP751sw.
  • Keywords
    Macrocycle , x-ray , BACE
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2006
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    796342