Thursday, November 14, 2013
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Ferrous iron (FeII)-dependent
drug delivery system
Mouse studies suggest an FeII-dependent
delivery system could be useful for selectively targeting drugs to diseased
tissues. The system involves conjugating a drug to a linker molecule and a
1,2,4-trioxolane ring that undergoes fragmentation in the presence of FeII.
In Plasmodium berghei-infected mice, a conjugate carrying an
irreversible inhibitor of Plasmodium
dipeptidyl aminopeptidase 1
selectively targeted infected red blood cells and showed more persistent
inhibition of the parasitic enzyme than unconjugated inhibitor. In P.
berghei-infected mice, the conjugate decreased parasitemia and showed
increased safety compared with unconjugated inhibitor. Next steps include
developing an optimized version of the delivery system and evaluating it for
the delivery of drugs to treat malaria and cancer.
Published online Nov. 14, 2013
Patent application filed;
available for licensing from the University
of California, San Francisco Office of Innovation,
Technology & Alliances
Deu, E. et al. Proc.
Natl. Acad. Sci. USA; published online Oct. 21, 2013;
Contact: Matthew Bogyo, Stanford University School of
Medicine, Stanford, Calif.
Contact: Adam R. Renslo, University of California, San
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