Cargando…
A 4-cyano-3-methylisoquinoline inhibitor of Plasmodium falciparum growth targets the sodium efflux pump PfATP4
We developed a novel series of antimalarial compounds based on a 4-cyano-3-methylisoquinoline. Our lead compound MB14 achieved modest inhibition of the growth in vitro of the human malaria parasite, Plasmodium falciparum. To identify its biological target we selected for parasites resistant to MB14....
Autores principales: | Gilson, Paul R., Kumarasingha, Rasika, Thompson, Jennifer, Zhang, Xinxin, Penington, Jocelyn Sietsma, Kalhor, Robabeh, Bullen, Hayley E., Lehane, Adele M., Dans, Madeline G., de Koning-Ward, Tania F., Holien, Jessica K., Soares da Costa, Tatiana P., Hulett, Mark D., Buskes, Melissa J., Crabb, Brendan S., Kirk, Kiaran, Papenfuss, Anthony T., Cowman, Alan F., Abbott, Belinda M. |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2019
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6635429/ https://www.ncbi.nlm.nih.gov/pubmed/31311978 http://dx.doi.org/10.1038/s41598-019-46500-5 |
Ejemplares similares
-
Optimization of
2,3-Dihydroquinazolinone-3-carboxamides
as Antimalarials Targeting PfATP4
por: Ashton, Trent D., et al.
Publicado: (2023) -
A G358S mutation in the Plasmodium falciparum Na(+) pump PfATP4 confers clinically-relevant resistance to cipargamin
por: Qiu, Deyun, et al.
Publicado: (2022) -
The malaria parasite cation ATPase PfATP4 and its role in the mechanism of action of a new arsenal of antimalarial drugs
por: Spillman, Natalie Jane, et al.
Publicado: (2015) -
PfATP4 inhibitors in the Medicines for Malaria Venture Malaria Box and Pathogen Box block the schizont-to-ring transition by inhibiting egress rather than invasion
por: Barnes, Claudia B. G., et al.
Publicado: (2022) -
Na(+) Regulation in the Malaria Parasite Plasmodiumfalciparum Involves the Cation ATPase PfATP4 and Is a Target of the Spiroindolone Antimalarials
por: Spillman, Natalie J., et al.
Publicado: (2013)