Main Area of Interest
Malaria remains an extremely widespread and devastating disease. Its toll on human life, economic development and social cohesion world-wide is matched by very few other infections. Prevention and treatment of malaria relies largely on the use of drugs and will continue to do so for some years. The case for new drugs, especially those having chemical structures distinct from the drugs in use and aimed at targets in the parasite cell that have not been previously exploited, has been persuasively stated many times over. This case becomes ever stronger as resistance to existing drugs continues to spread.
The microtubular system is a vital component of the most common and lethal malarial parasite Plasmodium falciparum during its development in its human host. Tubulins, the primary constituents of microtubules, may be promising drug targets, but the binding sites for potential tubulin-binding drugs in this organism are unknown. My project investigates the location and molecular architecture of a parasite-selective ligand-binding site on P. falciparum tubulin that might be exploited in the design of potent and selective new antimalarial agents. In addition to this work, I also use both two-dimensional and three-dimensional ligand-based virtual screening methods to identify novel anti-malarial tubulin-targetting scaffolds with the ultimate view to developing structure-activity relationships around this data.
History:
B.A. Mod. (TCD '08)Graduate Student (Oct 2008-Current)
Publications
1) Knox AJ, Price T, Pawlak M, Golfis G, Flood CT, Fayne D, Williams DC, Meegan MJ, Lloyd DG.
Integration of ligand and structure-based virtual screening for the identification of the first dual targeting agent for heat shock protein 90 (Hsp90) and tubulin.
J. Med. Chem., 2009, 52, 2177-80. [Read]
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