Issue 5, 2016

Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

Abstract

Design, synthesis and evaluation of very potent and selective β-secretase 2 (memapsin 1, BACE 2) inhibitors are described. The inhibitors were designed specifically to interact with the S2′-site of β-secretase 2 to provide >170 000-fold selectivity over β-secretase (BACE 1) and >15 000-fold selectivity over cathepsin D. BACE 2 is implicated in type 2 diabetes. The studies serve as an important guide to selective BACE 2 inhibitors.

Graphical abstract: Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

Supplementary files

Article information

Article type
Edge Article
Submitted
30 Sep 2015
Accepted
20 Jan 2016
First published
04 Feb 2016
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2016,7, 3117-3122

Author version available

Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

A. K. Ghosh, B. S. Reddy, Y. Yen, E. L. Cárdenas, K. V. Rao, D. Downs, X. Huang, J. Tang and A. D. Mesecar, Chem. Sci., 2016, 7, 3117 DOI: 10.1039/C5SC03718B

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