Article
Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines.
Nature communications - 12 Jan 2021
Sharma Manmohan, Malhotra Nipun, Yogavel Manickam, Harlos Karl, Melillo Bruno, Comer Eamon, Gonse Arthur, Parvez Suhel, Mitasev Branko, Fang Francis G, Schreiber Stuart L, Sharma Amit
Abstract excerpt
The inhibition of Plasmodium cytosolic phenylalanine tRNA-synthetase (cFRS) by a novel series of bicyclic azetidines has shown the potential to prevent malaria transmission, provide prophylaxis, and offer single-dose cure in animal models of malaria. To date, however, the molecular basis of Plasmodium cFRS inhibition by bicyclic azetidines has remained unknown. Here, we present structural and biochemical evidence...
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