Human p38 mitogen-activated protein kinase inhibitor drugs inhibit Plasmodium falciparum replication.
Exp Parasitol
; 128(2): 170-5, 2011 Jun.
Article
en En
| MEDLINE
| ID: mdl-21338604
We recently demonstrated that human p38 mitogen-activated protein kinase (MAPK) inhibitors reduced in vitro and in vivo replication of the protozoan parasites Toxoplasma gondii and Encephalitozoon cuniculi. In this study, we assessed the efficacy of five p38 MAPK inhibitors to block the replication of Plasmodium falciparum in human erythrocytes cultured ex vivo and demonstrate that the pyridinylimidazole RWJ67657 and the pyrrolobenzimidazole RWJ68198 reduced P. falciparum replication, yielded trophozoites that were greatly diminished in size at 24h, and that these two agents interfered with stage differentiation. Interestingly, the chloroquine-resistant strain W2 was significantly more sensitive to these drugs than was the chloroquine-sensitive strain HB3. These results suggest that pyridinylimidazoles and pyrrolobenzimidazoles designed to inhibit human p38 MAPK activation can be developed to treat malaria.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Plasmodium falciparum
/
Proteínas Quinasas p38 Activadas por Mitógenos
/
Inhibidores de Proteínas Quinasas
/
Antimaláricos
Límite:
Humans
Idioma:
En
Revista:
Exp Parasitol
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos