Ferrous iron-dependent delivery of therapeutic agents to the malaria parasite.

ABSTRACT:

Background

The malaria parasites Plasmodium falciparum and Plasmodium vivax generate significant concentrations of free unbound ferrous iron heme as a side product of hemoglobin degradation. The presence of these chemically reactive forms of iron, rare in healthy cells, presents an opportunity for parasite-selective drug delivery. Accordingly, our group is developing technologies for the targeted delivery of therapeutics to the intra-erythrocytic malaria parasite. These so-called 'fragmenting hybrids' employ a 1,2,4-trioxolane ring system as an iron(II)-sensing 'trigger' moiety and a 'traceless' retro-Michael linker to which a variety of partner drug species may be attached. After ferrous iron-promoted activation in the parasite, the partner drug is released via a β-elimination rea

SUBMITTER: Mahajan SS 

PROVIDER: S-EPMC3574796 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature