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Starving the Malaria Parasite: Inhibitors Active against the Aspartic Proteases Plasmepsins I, II, and IV
Author(s) -
Hof Fraser,
Schütz Andri,
Fäh Christoph,
Meyer Solange,
Bur Daniel,
Liu Jun,
Goldberg Daniel E.,
Diederich François
Publication year - 2006
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200504119
Subject(s) - protease , chemistry , biochemistry , active site , malaria , biology , enzyme , immunology
Clamping down : A new class of aspartic protease inhibitors that target the malarial protease family Plasmepsin are reported. These ligands utilize a novel “diamine clamp” to engage the catalytic dyad. They are potent inhibitors of plasmepsins I, II, and IV, while retaining good selectivity against the closely related human cathepsins D and E.