Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies

Given that many antifungal medications are susceptible to evolved resistance, there is a need for novel drugs with unique mechanisms of action. Inhibiting the essential proton pump Pma1p, a P-type ATPase, is a potentially effective therapeutic approach that is orthogonal to existing treatments. We i...

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Detalles Bibliográficos
Autores principales: Ottilie, Sabine, Goldgof, Gregory M., Cheung, Andrea L., Walker, Jennifer L., Vigil, Edgar, Allen, Kenneth E., Antonova-Koch, Yevgeniya, Slayman, Carolyn W., Suzuki, Yo, Durrant, Jacob D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2018
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5820243/
https://www.ncbi.nlm.nih.gov/pubmed/29464421
http://dx.doi.org/10.1186/s13321-018-0261-3
Descripción
Sumario:Given that many antifungal medications are susceptible to evolved resistance, there is a need for novel drugs with unique mechanisms of action. Inhibiting the essential proton pump Pma1p, a P-type ATPase, is a potentially effective therapeutic approach that is orthogonal to existing treatments. We identify NSC11668 and hitachimycin as structurally distinct antifungals that inhibit yeast ScPma1p. These compounds provide new opportunities for drug discovery aimed at this important target. [Image: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1186/s13321-018-0261-3) contains supplementary material, which is available to authorized users.

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