Malaria, a life-threatening disease caused by parasites of the genus Plasmodium, affects 500 million people annually, of which more than one million die. [1] The emergence of multi-drugresistant strains of Plasmodium falciparum, the parasite that causes the deadliest form of malaria, exacerbates the
De novo Disign, Synthesis, and in vitro Evaluation of a New Class of Nonpeptidic Inhibitors of the Malarial Enzyme Plasmepsin II.
✍ Scribed by David A. Carcache; Simone R. Hoertner; Andreas Bertogg; Christoph Binkert; Daniel Bur; Hans Peter Maerki; Arnulf Dorn; Francois Diederich
- Publisher
- John Wiley and Sons
- Year
- 2003
- Weight
- 54 KB
- Volume
- 34
- Category
- Article
- ISSN
- 0931-7597
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## 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 re
## Abstract A new class of nonpeptidic inhibitors of the malarial aspartic protease plasmepsin II (PMII) with up to single‐digit micromolar activities (__IC__~50~ values) was developed by structure‐based __de novo__ design. The active‐site matrix used in the design was based on an X‐ray crystal str
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