Submitted on November 1, 2005
Revised on December 6, 2005
Accepted on December 6, 2005
Fighting parasitic disease by blocking protein farnesylation
Richard T. Eastman, Frederick S. Buckner, Kohei Yokoyama, Michael H. Gelb, and Wesley C. Van Voorhis
University of Washington, Seattle, WA 98195-7185
Corresponding Author: richeast{at}u.washington.edu
Protein prenylation is a form of post-translational modification that occurs in most, if not all, eukaryotic cells. Protein farnesyltransferase inhibitors (PFTIs) have been developed as anti-cancer chemotherapeutics. Recent studies have investigated the use of protein prenylation inhibitors for the treatment of eukaryotic pathogens. To accelerate progress in the development of therapeutics for protozoan parasitic diseases, researchers are applying the knowledge gained from developing PFTIs for cancer treatment to the potential use as anti-parasitic agents. Inhibitors of protein farnesyltransferase have already been shown to be efficacious in the treatment of eukaryotic pathogens in animal models, including Trypanosoma brucei and Plasmodium falciparum. Here, we summarize the current evidence and progress that supports targeting prenylation enzymes for the treatment of parasitic diseases.
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