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Issue 5, 2016
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Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

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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

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Publication details

The article was received on 30 sep. 2015, accepted on 20 jan. 2016 and first published on 04 feb. 2016


Article type: Edge Article
DOI: 10.1039/C5SC03718B
Citation: Chem. Sci., 2016,7, 3117-3122
  • Open access: Creative Commons BY-NC license
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    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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