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Experimentsl Therapeutics: Lipophilic Bisphosphonates Are Potent Inhibitors of Plasmodium Liver-Stage Growth

June 18, 2010 - 09:41 -- Kabogo Ndegwa
Author(s): 
Agam Prasad Singh, Yonghui Zhang, Joo-Hwan No, Roberto Docampo, Victor Nussenzweig, and Eric Oldfield
Reference: 
Antimicrobial Agents and Chemotherapy, July 2010, p. 2987-2993, Vol. 54, No. 7

Nitrogen-containing bisphosphonates, drugs used to treat bone resorption diseases, also have activity against a broad range of protists, including blood-stage Plasmodium spp. Here, we show that new-generation "lipophilic" bisphosphonates designed as anticancer agents that block protein prenylation also have potent activity against Plasmodium liver stages, with a high (>100) therapeutic index.

Redefining the role of de novo fatty acid synthesis in Plasmodium parasites.

November 18, 2009 - 12:36 -- Kabogo Ndegwa
Author(s): 
Alice S. Tarun, Ashley M. Vaughan, Stefan H.I. Kappe.
Reference: 
Trends in Parasitology, Volume 25, Issue 12, December 2009, Pages 545-550, doi:10.1016/j.pt.2009.09.002

Fatty acids are essential components of membranes, and are also involved in cell signalling. Plasmodium, the parasite that causes malaria, scavenges fatty acids from its hosts. However, Plasmodium also possesses enzymes for a prokaryotic-like de novo fatty acid synthesis pathway, which resides in the apicoplast. Recent research has demonstrated that Plasmodium parasites depend on de novo fatty acid synthesis only for liver-stage development.

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