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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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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:
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
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author 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.
author_facet 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.
author_sort Ottilie, Sabine
collection PubMed
description 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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spelling pubmed-58202432018-02-27 Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies 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. J Cheminform Research Article 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. Springer International Publishing 2018-02-20 /pmc/articles/PMC5820243/ /pubmed/29464421 http://dx.doi.org/10.1186/s13321-018-0261-3 Text en © The Author(s) 2018 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Article
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.
Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies
title Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies
title_full Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies
title_fullStr Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies
title_full_unstemmed Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies
title_short Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies
title_sort two inhibitors of yeast plasma membrane atpase 1 (scpma1p): toward the development of novel antifungal therapies
topic Research Article
url 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
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