司马西特

生物活性

Semagacestat(LY450139) is a γ-secretase blocker with an IC50 of 15 nM.β-amyloid is a peptide of 39 to 43 amino acids. ^[1] The isoforms with 40 and 42 amino acids (Aβ40/42) are the main constituents of amyloid plaques in the brains of Alzheimer’s disease patients. β-amyloid is formed by proteolysis of APP. Research on laboratory rats suggest that the soluble form of this peptide is a causative agent in the development of Alzheimer’s. Semagacestat blocks the enzyme γ-secretase, which (along with β-secretase) is responsible for APP proteolysis. ^[2

参考文献

[1] Kreft AF et al. J Med Chem. 2009 Oct 22;52(20):6169-88.