Drug Discovery reported the identification of a novel anti-malarial drug target recently. A team of scientists from Department of Pediatrics, University of California, San Diego School of Medicine report the identification of inhibitors of one of the key enzymes involves in survival of malarial parasite (causative agent of malaria). The new target may open up new avenues for anti-malarial drugs and help in controlling the menace of malaria worldwide. The study has been published in the Journal of Medicinal Chemistry.
Malaria kills over 1.2 million people every year. Eradication of malaria has not met with significant success since parasite manages to develop resistance to drugs and the lack of vaccines for the disease adds to malaria woes across the world.
The team of scientists first conducted high-throughput screening of 350,000 compounds in National Institutes of Health’s Molecular Libraries Small Molecule Repository (MLSMR) and identified compounds that inhibited enzymes which plays important role in parasite development. They identified Plasmodium falciparum glucose-6-phosphate dehydrogenase (PfG6PD), responsible for proliferation and propagation of P.falciparum. The parasitic form of the enzyme G6PD of Plasmodium falciparum is responsible for maximum G6PD activity in red blood cells that are infected.
The team identified ML276 as the first reported selective inhibitor of PfG6PD. The inhibitor stops growth of malarial parasites in cultured RBCs.
ML276 is a potent anti-malaria drug target.
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