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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters