Development of a New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 7??Azabicyclo [2.2. 1] heptane Scaffold

…, SR Hörtner, P Seiler, F Diederich, A Dorn…

Index: Carcache, David A.; Hoertner, Simone R.; Seiler, Paul; Diederich, Francois; Dorn, Arnulf; Maerki, Hans Peter; Binkert, Christoph; Bur, Daniel Helvetica Chimica Acta, 2003 , vol. 86, # 6 p. 2173 - 2191

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Citation Number: 27

Abstract

Abstract Plasmepsin II (PMII), a malarial aspartic protease involved in the catabolism of hemoglobin in parasites of the genus Plasmodium, and renin, a human aspartic protease, share 35% sequence identity in their mature chains. Structures of 4-arylpiperidine inhibitors complexed to human renin were reported by Roche recently. The major conformational changes, compared to a structure of renin, with a peptidomimetic inhibitor were identified ...