Targeting the plasmepsin 4 orthologs of Plasmodium sp with "Double Drug" inhibitors

Janka, L., Clemente, J., Vaiana, N., Sparatore, A., Romeo, S. and Dunn, B.M. (2008) Targeting the plasmepsin 4 orthologs of Plasmodium sp with "Double Drug" inhibitors. Protein and Peptide Letters, 15 (9). pp. 868-873. ISSN 0929-8665 doi: 10.2174/092986608785849218

Abstract/Summary

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.