Targeting the Plasmepsin 4 Orthologs of Plasmodium sp. with “Double Drug” Inhibitors

Author(s): Linda Janka, Jose Clemente, N. Vaiana, A. Sparatore, Sergio Romeo, Ben M. Dunn.

Journal Name: Protein & Peptide Letters

Volume 15 , Issue 9 , 2008

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Abstract:

Plasmepsin 4 (PM4) is a digestive vacuole enzyme found in all Plasmodium species examined to date. While P. falciparum has three additional aspartic proteinases in its digestive vacuole in addition to plasmepsin 4, other Plasmodium species have only PM4 in their digestive vacuole. Therefore, PM4 may be a good target for the development of an antimalarial drug. This study presents data obtained with PM4s from several Plasmodium species. Low nanomolar Ki values have been observed for all PM4s studied.

Keywords: Plasmepsin, proteolytic enzyme from the Plasmodium species, a word derived from Plasmodium pepsin, Double Drug, a combination of two molecular entities in one compound that kill a pathogen by two mechanisms, statine, the naturallyoccurring amino acid derivative (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid, antimalarial, a compound that blocks the growth of the malarial parasite in culture, Proenzyme

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Article Details

VOLUME: 15
ISSUE: 9
Year: 2008
Page: [868 - 873]
Pages: 6
DOI: 10.2174/092986608785849218
Price: $65

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