Malaria is a parasitic condition caused by the Plasmodium falciparum parasite and remains one of the leading causes of mortality in developing nations. In particular, residents of sub-Saharan and South East Asian countries are at high risk of contracting this parasitic condition. Over the years, a tremendous effort has yielded considerable progress to eliminate and eventually eradicate this condition, largely through the development of effective therapeutics. However, in the long run, most antibiotics designed to treat malarial infections prove ineffective. This is largely due to the generation of Plasmodium parasites that have gained resistance to these antibiotics.
Now, a new study published in the journal, Science Translational Medicine led by Margaret Phillips and Susan Charman at the University of Texas Southwestern Medical Center and Monash University respectively, report the development of a new parasite inhibitor, DM265. Their investigations revealed that DM265 is able to inhibit a key protein known as DHODH (dihydroorotate dehydrogenase). This protein resides within one of the cell’s sub-compartments known as the mitochondrion, which is often called the cell’s powerhouse since it is responsible for generating the majority of cellular energy. Not surprisingly, humans also contain DHODH but fortunately, the plasmodium and human proteins differ in their sequence. It was this molecular distinction that motivated the researchers to develop an inhibitor for the plasmodium DHODH.
The Texan and Australian scientists discovered that the DM265 molecule lodges and locks itself into an important region of the DHODH protein molecule, thus interfering with its function. Furthermore, the team discovered that the DM265 molecule represents minimal-to-none toxic side effects and also doesn’t interfere with normal heart functions, which can be a leading cause of concern for certain drugs. Moreover, the team conducted exhaustive studies in mammals, namely dogs and mice, and concluded that there were no toxic or harmful side effects of this drug. In addition, the drug requires non-daily dosing, owing to its prolonged half-life spanning up to three days.
Owing largely to the progress outlined in this landmark study, DM265 has proceeded into human trials and it is hoped that it will be approved for use in the very near future.
References:
http://www.utsouthwestern.edu/newsroom/news-releases/year-2015/july/researchers-find-cure-for-malaria.html
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