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Structure and Modeling in the Design of b- and c-Secretase Inhibitors

Holloway, M. Katharine, Hunt, Peter and McGaughey, Georgia B. (2009) Structure and Modeling in the Design of b- and c-Secretase Inhibitors. Drug Development Research, 70 (2). pp. 70-93.


This review discusses the involvement of structure and modeling in the design of -secretase (BACE-1) and -secretase inhibitors as putative Alzheimer's Disease therapeutics. The early and broad availability of structural information for BACE-1, a membrane-tethered aspartyl protease, has led to the use of in silico methods in the overall design and optimization process. However, for -secretase, an integral membrane protein, the lack of a detailed 3D structure has limited the application of computational methods.

Item Type: Article
Additional Information: archiving not allowed on institutional repository
Keywords: Alzheimer's disease; beta-secretase; BACE-1; gamma-secretase; structure-based design
Date Deposited: 14 Dec 2009 13:47
Last Modified: 14 Dec 2009 13:47


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