期刊
CURRENT DRUG TARGETS
卷 8, 期 1, 页码 3-13出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138945007779315551
关键词
malaria; apicoplast; isoprenoid biosynthesis; DOXP reductoisomerase; fosmidomycin; FR900098
In Plasmodium falciparum the biosynthesis of isoprenoids is achieved by die mevalonate-independent 1-deoxy-D-Xylulose 5-phosphate (DOXP) pathway. The enzymes of the DOXP pathway are localised inside the plastid-like organelle (apicoplast). Fosmidomycin inhibits DOXP reductoisomerase, the second enzyme of this pathway. The antimalarial activity of fosmidomycin was established in vitro and in a rodent malaria model. Fosmidomycin alone or in combination with clindamycin was evaluated for the treatment of acute uncomplicated P. falciparum malaria in early phase 11 studies. Fosmidomycin monotherapy led to a fast parasite and fever clearance but was inefficient in radical elimination of the parasites. With the fosmidomycin-clindamycin combinations the cure ratio on day 28 was 100 % (10/10) with treatment durations of 5 and 4 days. The cure ratio was 90 % (9/10) with treatment duration of 3 days.
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