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.
Keywords: Plasmepsin, aspartic protease inhibitor, antimalarial, drug discovery, medicinal chemistry, Abstract: Plasmepsins, hemoglobin degradation, plasmepsin inhibitors as, target druggability, non-digestive vacuole plasmepsins
Current Topics in Medicinal Chemistry
Title: Recent Advances in Plasmepsin Medicinal Chemistry and Implications for Future Antimalarial Drug Discovery Efforts
Volume: 12 Issue: 5
Author(s): Marvin J. Meyers and Daniel E. Goldberg
Affiliation:
Keywords: Plasmepsin, aspartic protease inhibitor, antimalarial, drug discovery, medicinal chemistry, Abstract: Plasmepsins, hemoglobin degradation, plasmepsin inhibitors as, target druggability, non-digestive vacuole plasmepsins
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.
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Cite this article as:
J. Meyers Marvin and E. Goldberg Daniel, Recent Advances in Plasmepsin Medicinal Chemistry and Implications for Future Antimalarial Drug Discovery Efforts, Current Topics in Medicinal Chemistry 2012; 12 (5) . https://dx.doi.org/10.2174/156802612799362959
DOI https://dx.doi.org/10.2174/156802612799362959 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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