Discovery of a subnanomolar helical D-tridecapeptide inhibitor of γ-secretase

被引：46

作者：

Bihel, F

Das, C

Bowman, MJ

Wolfe, MS

机构：

[1] Harvard Univ, Sch Med, Ctr Neurol Dis, Boston, MA 02115 USA

[2] Brigham & Womens Hosp, Boston, MA 02115 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 16期

关键词：

D O I：

10.1021/jm049788c

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

gamma-Secretase is the second of two proteolytic enzymes responsible for the release of the amyloid beta-peptide implicated in the etiology of Alzheimer's disease. Here, we used solid-phase synthesis to generate a new series of helical peptides as gamma-secretase inhibitors, one of which, 11, showed an IC50 of 140 muM in a cell-free enzyme assay.

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页码：3931 / 3933

页数：3

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