Document Report Card
Basic Information
ID: ALA1147464
Journal: Bioorg Med Chem Lett
Title: Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.
Authors: Hu B, Fan KY, Bridges K, Chopra R, Lovering F, Cole D, Zhou P, Ellingboe J, Jin G, Cowling R, Bard J.
Abstract: A new series of bis-statine based peptidomimetic inhibitors of human beta-secretase (BACE 1) was developed by structure-based modification of the three regions to the initial lead 3: an N-terminus, a central bis-statine core, and a C-terminus. Introduction of a 4-aminomethylbenzoic acid on the C-terminus resulted in a potent BACE 1 inhibitor with an IC50 value of 21 nM. The general requirements for the optimal substrate-enzyme interaction are disclosed herein.
CiteXplore: 15177452