Abstract
As beta-secretase, memapsin 2 cleaves amyloid-beta precursor protein, which leads ultimately to the onset of Alzheimer's disease. As such, memapsin 2 is an excellent target of inhibitor drugs for the treatment of this disease. Here we describe the tools for memapsin 2 inhibitor design that have been developed and results from the structure-based inhibitor design. Strategy for the design of memapsin 2 inhibitors with pharmaceutical potential is also discussed.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Alzheimer Disease / drug therapy*
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Amyloid Precursor Protein Secretases
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Aspartic Acid Endopeptidases / metabolism*
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Crystallography, X-Ray
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Drug Design
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Endopeptidases
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Humans
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Oligopeptides / chemistry
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Oligopeptides / therapeutic use*
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Protease Inhibitors / chemistry*
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Protease Inhibitors / pharmacology*
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Protease Inhibitors / therapeutic use
Substances
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OM99-2
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Oligopeptides
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Protease Inhibitors
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Amyloid Precursor Protein Secretases
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Endopeptidases
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Aspartic Acid Endopeptidases
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BACE1 protein, human