Abstract
Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addressing the known ones. As proteases in general have been proven to be excellent drug targets and the development of inhibitors has frequently resulted in approved drugs, this review will only focus on the proteases of Plasmodium falciparum as drug targets. The completion of the sequencing of the Plasmodium falciparum genome in 2002 lead to the discovery of nearly 100 putative proteases encoded therein. Within this review, only those proteases and inhibitors thereof will be discussed in more detail, in which their biological function has been determined undoubtedly or in those cases, in which the development of specific inhibitors has significantly contributed to the understanding of the underlying biological role of the respective protease thus validating the role as promising drug target.
Keywords: Malaria, Plasmepsin, Falcipain, protease inhibitors
Current Topics in Medicinal Chemistry
Title: Proteases of Plasmodium falciparum as Potential Drug Targets and Inhibitors Thereof
Volume: 10 Issue: 3
Author(s): Christof Wegscheid-Gerlach, Hans-Dieter Gerber and Wibke E. Diederich
Affiliation:
Keywords: Malaria, Plasmepsin, Falcipain, protease inhibitors
Abstract: Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addressing the known ones. As proteases in general have been proven to be excellent drug targets and the development of inhibitors has frequently resulted in approved drugs, this review will only focus on the proteases of Plasmodium falciparum as drug targets. The completion of the sequencing of the Plasmodium falciparum genome in 2002 lead to the discovery of nearly 100 putative proteases encoded therein. Within this review, only those proteases and inhibitors thereof will be discussed in more detail, in which their biological function has been determined undoubtedly or in those cases, in which the development of specific inhibitors has significantly contributed to the understanding of the underlying biological role of the respective protease thus validating the role as promising drug target.
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Wegscheid-Gerlach Christof, Gerber Hans-Dieter and Diederich E. Wibke, Proteases of Plasmodium falciparum as Potential Drug Targets and Inhibitors Thereof, Current Topics in Medicinal Chemistry 2010; 10 (3) . https://dx.doi.org/10.2174/156802610790725461
DOI https://dx.doi.org/10.2174/156802610790725461 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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