Validation of Plasmodium falciparum dUTPase as the target of 5′-tritylated deoxyuridine analogues with anti-malarial activity

[Background] Malaria remains as a major global problem, being one of the infectious diseases that engender highest mortality across the world. Due to the appearance of resistance and the lack of an effective vaccine, the search of novel anti-malarials is required. Deoxyuridine 5′-triphosphate nucleo...

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Detalles Bibliográficos
Autores: Pérez-Moreno, Guiomar, Sánchez-Carrasco, Paula, Ruiz-Pérez, Luis Miguel, Johansson, N.G., Müller, Sylke, Baragaña, Beatriz, Hampton, Shahienaz, Gilbert, Ian H., Kaiser, Marcel, Sarkar, Sandipan, Pandurangan, Thiyagamurthy, Kumar, Vijeesh, González-Pacanowska, Dolores
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/196266
Acceso en línea:http://hdl.handle.net/10261/196266
Access Level:acceso abierto
Palabra clave:lasmodium falciparum
Deoxyuridine 5′-triphosphate nucleotido-hydrolase
5′-tritylated deoxyuridine analogues
Mode of action
Descripción
Sumario:[Background] Malaria remains as a major global problem, being one of the infectious diseases that engender highest mortality across the world. Due to the appearance of resistance and the lack of an effective vaccine, the search of novel anti-malarials is required. Deoxyuridine 5′-triphosphate nucleotido-hydrolase (dUTPase) is responsible for the hydrolysis of dUTP to dUMP within the parasite and has been proposed as an essential step in pyrimidine metabolism by providing dUMP for thymidylate biosynthesis. In this work, efforts to validate dUTPase as a drug target in Plasmodium falciparum are reported.