527674-87-9Relevant academic research and scientific papers
Structure-based design: Potent inhibitors of human brain memapsin 2 (β-secretase)
Ghosh,Bilcer,Harwood,Kawahama,Shin,Hussain,Hong,Loy,Nguyen,Koelsch,Ermolieff,Tang
, p. 2865 - 2868 (2007/10/03)
Memapsin 2 (β-secretase) is one of two proteases that cleave the β-amyloid precursor protein (APP) to produce the 40-42 residue amyloid-β peptide (Aβ) in the human brain, a key event in the progression of Alzheimer's disease. On the basis of the X-ray crystal structure of our lead inhibitor (2, OM99-2 with eight residues) bound to memapsin, we have reduced the molecular weight and designed potent memapsin inhibitors. Structure-based design and preliminary structure-activity studies have been presented.
