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4 October 2000. Researchers announced a step forward in the rational design of drugs to inhibit
β-secretase (also called memapsin 2 and BACE) with the publication in tomorrow's
Science of the crystal structure of the enzyme locked in a complex with a novel
inhibitor. The inhibitor, called OM99-2, complexes to an eight-residue structure
in the active site of the enzyme. Information about the enzyme's active site will
aid researchers in designing small molecule candidates for drugs aimed at blocking
β-amyloid production through inhibition of β-secretase.-June Kinoshita.
Reference:Hong L, Koelsch G, Lin X, Wu S, Tang J, Terzyan S, Zhang C, Ghosh A. Structure of the protease domain of memapsin 2 (b-secretase) complexed
with inhibitor. Science 2000 Oct 6;290(5489):150-3. Abstract
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Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor.
