Starving the malaria parasite: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV

Fraser Hof; Andri Schütz; Christoph Fäh; Solange Meyer; Daniel Bur; Jun Liu; Daniel E. Goldberg; François Diederich

doi:10.1002/anie.200504119

Starving the malaria parasite: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV

Fraser Hof
, Andri Schütz
, Christoph Fäh
, Solange Meyer
, Daniel Bur
, Jun Liu
, Daniel E. Goldberg
, François Diederich

Research output: Contribution to journal › Article › peer-review

83 Scopus citations

Abstract

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. (Chemical Equation Presented) .

Original language	English
Pages (from-to)	2138-2141
Number of pages	4
Journal	Angewandte Chemie - International Edition
Volume	45
Issue number	13
DOIs	https://doi.org/10.1002/anie.200504119
State	Published - Mar 20 2006

Keywords

Aspartic proteases
Drug design
Inhibitors
Malaria
Medicinal chemistry

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10.1002/anie.200504119

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abstract = "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. (Chemical Equation Presented) .",

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AU - Hof, Fraser

AU - Schütz, Andri

AU - Fäh, Christoph

AU - Meyer, Solange

AU - Bur, Daniel

AU - Liu, Jun

AU - Goldberg, Daniel E.

AU - Diederich, François

PY - 2006/3/20

Y1 - 2006/3/20

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KW - Aspartic proteases

KW - Drug design

KW - Inhibitors

KW - Malaria

KW - Medicinal chemistry

UR - https://www.scopus.com/pages/publications/33746276423

U2 - 10.1002/anie.200504119

DO - 10.1002/anie.200504119

M3 - Article

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AN - SCOPUS:33746276423

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JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 13

ER -

Starving the malaria parasite: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV

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Keywords

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