Memapsin 2 (beta-secretase) as a therapeutic target.
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.
Protein Studies Program, Oklahoma Medical Research Foundation, Oklahoma City, OK, USA.
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Hong
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Turner
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Koelsch
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Ghosh
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Tang
D000544:Alzheimer Disease / Q000188:drug therapy*; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases / Q000378:metabolism*; D018360:Crystallography, X-Ray; D015195:Drug Design; D010450:Endopeptidases; D006801:Humans; D009842:Oligopeptides / Q000737:chemistry / Q000627:therapeutic use*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use
C414614:OM99-2; D009842:Oligopeptides; D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases; D010450:Endopeptidases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human