Article
Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase.
European journal of medicinal chemistry - 1 Aug 2011
Recio Eliseo, Musso-Buendía Alexander, Vidal Antonio E, Ruda Gian Filippo, Kasinathan Ganasan, Nguyen Corinne, Ruiz-Pérez Luis Miguel, Gilbert Ian H, González-Pacanowska Dolores
Abstract excerpt
We have previously identified a series of triphenylmethane derivatives of deoxyuridine with antimalarial activity in vitro which selectively inhibit Plasmodium falciparum deoxyuridine triphosphate nucleotidohydrolase (PfdUTPase) compared to the human enzyme. The crystal structure of PfdUTPase in complex with one of these inhibitors suggested that the triphenylmethane derivative was selective due to a series of...
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