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Recent Advances in the Discovery of Haem-Targeting Drugs for Malaria and Schistosomiasis
University of Stellenbosch, Private Bag X1, Matieland 7602, South Africa
University of Cape Town, Private Bag, Rondebosch 7701, South Africa
* Author to whom correspondence should be addressed.
Received: 30 June 2009; in revised form: 20 July 2009 / Accepted: 22 July 2009 / Published: 4 August 2009
Abstract: Haem is believed to be the target of some of the historically most important antimalarial drugs, most notably chloroquine. This target is almost ideal as haem is host-derived and the process targeted, haemozoin formation, is a physico-chemical process with no equivalent in the host. The result is that the target remains viable despite resistance to current drugs, which arises from mutations in parasite membrane transport proteins. Recent advances in high-throughput screening methods, together with a better understanding of the interaction of existing drugs with this target, have created new prospects for discovering novel haem-targeting chemotypes and for target-based structural design of new drugs. Finally, the discovery that Schistosoma mansoni also produces haemozoin suggests that new drugs of this type may be chemotherapeutic not only for malaria, but also for schistosomiasis. These recent developments in the literature are reviewed.
Keywords: haem; haemozoin; high-throughput screening; rational drug design
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De Villiers, K.A.; Egan, T.J. Recent Advances in the Discovery of Haem-Targeting Drugs for Malaria and Schistosomiasis. Molecules 2009, 14, 2868-2887.
De Villiers KA, Egan TJ. Recent Advances in the Discovery of Haem-Targeting Drugs for Malaria and Schistosomiasis. Molecules. 2009; 14(8):2868-2887.
De Villiers, Katherine A.; Egan, Timothy J. 2009. "Recent Advances in the Discovery of Haem-Targeting Drugs for Malaria and Schistosomiasis." Molecules 14, no. 8: 2868-2887.