Design of potent inhibitors for human brain memapsin 2 (β-secretase) [1]

Journal of the American Chemical Society

Volumn 122, Issue 14, 2000, Pages 3522-3523

  Ghosh, Arun K ^a   Shin, Dongwoo ^b   Downs, Debbie ^c   Koelsch, Gerald ^c   Lin, Xinli ^c   Ermolieff, Jacques ^c   Tang, Jordan ^c  

^a UNIVERSITY OF ILLINOIS AT CHICAGO   (United States)

^b OKLAHOMA MEDICAL RESEARCH FOUNDATION   (United States)

^c UNIVERSITY OF OKLAHOMA COLLEGE OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA SECRETASE; ENZYME INHIBITOR; OM 99 1; OM 99 2; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; BRAIN; CONTROLLED STUDY; DRUG SYNTHESIS; ENZYME BINDING; ENZYME INHIBITOR INTERACTION; HUMAN; INHIBITION KINETICS; LETTER; STRUCTURE ACTIVITY RELATION;

EID: 0034639925     PISSN: 00027863     EISSN: None     Source Type: Journal    
DOI: 10.1021/ja000300g     Document Type: Letter

References (18)

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17. Memapsin 2 inhibition was measured using recombinant enzyme produced from E. coli expression as described in ref 2. A fluorogenic substrate Arg-Glu(EDANS)-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(Dabcyl)-Argwas used with 0.47 μM of the enzyme in 0.1 M Na-acetate + 5% dimethyl sulfoxide, pH 4.5 at 37°C. The excitation wavelength was 350 nm and the emission wavelength was 490 nm. Details of this assay will be described elsewhere.
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