Targeting the plasmepsin 4 orthologs of Plasmodium sp. with "double drug" inhibitors

Linda Janka; Jose Clemente; N. Vaiana; A. Sparatore; Sergio Romeo; Ben M. Dunn

doi:10.2174/092986608785849218

Targeting the plasmepsin 4 orthologs of Plasmodium sp. with "double drug" inhibitors

Linda Janka, Jose Clemente, N. Vaiana, A. Sparatore, Sergio Romeo, Ben M. Dunn

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

7 Scopus citations

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 K_i values have been observed for all PM4s studied.

Original language	English
Pages (from-to)	868-873
Number of pages	6
Journal	Protein and Peptide Letters
Volume	15
Issue number	9
DOIs	https://doi.org/10.2174/092986608785849218
State	Published - Sep 2008
Externally published	Yes

Keywords

A combination of two molecular entities in one compound that kill a pathogen by two mechanisms
A word derived from plasmodium pepsin
Double drug
Plasmepsin
Proteolytic enzyme from the plasmodium species
Statine

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10.2174/092986608785849218

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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.",

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T1 - Targeting the plasmepsin 4 orthologs of Plasmodium sp. with "double drug" inhibitors

AU - Janka, Linda

AU - Clemente, Jose

AU - Vaiana, N.

AU - Sparatore, A.

AU - Romeo, Sergio

AU - Dunn, Ben M.

PY - 2008/9

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AB - 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.

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Targeting the plasmepsin 4 orthologs of Plasmodium sp. with "double drug" inhibitors

Abstract

Keywords

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