Recent advances in plasmepsin medicinal chemistry and implications for future antimalarial drug discovery efforts

Marvin J. Meyers, Daniel E. Goldberg

Research output: Contribution to journalEditorial

51 Scopus citations

Abstract

Plasmepsins are the aspartic proteases of Plasmodium that play key roles in the survival of the parasite in its host. The plasmepsins of the digestive vacuole play an important role in hemoglobin degradation, providing the parasite with a vital source of nutrients. Recently, plasmepsin V has been shown to be an essential protease, processing hundreds of parasite proteins for export into the host erythrocyte. The functions of the remaining plasmepsins have yet to be discovered. Over the past decade, much effort has been placed towards developing plasmepsin inhibitors as antimalarial agents, particularly targeting the digestive vacuole. This review will highlight some of the recent work in this field with a particular focus on target druggability and strategies for identifying plasmepsins inhibitors as effective antimalarial drugs. Given recent advances in understanding the fundamental roles of the various plasmepsins, it is likely that the most effective antimalarial plasmepsin targets will be the non-digestive vacuole plasmepsins.

Original languageEnglish
Pages (from-to)445-455
Number of pages11
JournalCurrent Topics in Medicinal Chemistry
Volume12
Issue number5
DOIs
StatePublished - Mar 1 2012

Keywords

  • Antimalarial
  • Aspartic protease inhibitor
  • Drug discovery
  • Medicinal chemistry
  • Plasmepsin

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