Abstract
Malaria, caused by parasites of the genus Plasmodium, leads to over half a million deaths per year, 90% of which are caused by Plasmodium falciparum. P. vivax usually causes milder forms of malaria; however, P. vivax can remain dormant in the livers of infected patients for weeks or years before re-emerging in a new bout of the disease. The only drugs available that target all stages of the parasite can lead to severe side effects in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency; hence, there is an urgent need to develop new drugs active against blood and liver stages of the parasite. Different groups have demonstrated that triclosan, a common antibacterial agent, targets the Plasmodium liver enzyme enoyl reductase. Here, we provide 4 independent lines of evidence demonstrating that triclosan specifically targets both wild-type and pyrimethamine-resistant P. falciparum and P. vivax dihydrofolate reductases, classic targets for the blood stage of the parasite. This makes triclosan an exciting candidate for further development as a dual specificity antimalarial, which could target both liver and blood stages of the parasite
Original language | English |
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Article number | 1038 |
Journal | Scientific Reports |
Volume | 8 |
Issue number | 1 |
Early online date | 18 Jan 2018 |
DOIs | |
Publication status | Published - 18 Jan 2018 |
Keywords
- Andes
- Argentina
- Chile
- climate change
- ENSO
- MOD10A1
- MODIS
- snow albedo
- snow cover extent
- time series analysis
- Enzyme Activation/drug effects
- Triclosan/chemistry
- Molecular Conformation
- Models, Molecular
- Structure-Activity Relationship
- Tetrahydrofolate Dehydrogenase/chemistry
- Protein Binding
- Plasmodium/drug effects
- Antimalarials/chemistry
- Binding Sites
- Folic Acid Antagonists/chemistry
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A robot scientist for drug design and chemical genetics
King, R. D.
01 Jan 2018
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