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

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Primary Papers

  1. . Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor. Science. 2000 Oct 6;290(5489):150-3. PubMed.