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ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans

The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substan...

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Autores principales: Youngsaye, Willmen, Hartland, Cathy L, Morgan, Barbara J, Ting, Amal, Nag, Partha P, Vincent, Benjamin, Mosher, Carrie A, Bittker, Joshua A, Dandapani, Sivaraman, Palmer, Michelle, Whitesell, Luke, Lindquist, Susan, Schreiber, Stuart L, Munoz, Benito
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Beilstein-Institut 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3740683/
https://www.ncbi.nlm.nih.gov/pubmed/23946849
http://dx.doi.org/10.3762/bjoc.9.171
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author Youngsaye, Willmen
Hartland, Cathy L
Morgan, Barbara J
Ting, Amal
Nag, Partha P
Vincent, Benjamin
Mosher, Carrie A
Bittker, Joshua A
Dandapani, Sivaraman
Palmer, Michelle
Whitesell, Luke
Lindquist, Susan
Schreiber, Stuart L
Munoz, Benito
author_facet Youngsaye, Willmen
Hartland, Cathy L
Morgan, Barbara J
Ting, Amal
Nag, Partha P
Vincent, Benjamin
Mosher, Carrie A
Bittker, Joshua A
Dandapani, Sivaraman
Palmer, Michelle
Whitesell, Luke
Lindquist, Susan
Schreiber, Stuart L
Munoz, Benito
author_sort Youngsaye, Willmen
collection PubMed
description The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure–activity relationships led to the discovery of ML212.
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spelling pubmed-37406832013-08-14 ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans Youngsaye, Willmen Hartland, Cathy L Morgan, Barbara J Ting, Amal Nag, Partha P Vincent, Benjamin Mosher, Carrie A Bittker, Joshua A Dandapani, Sivaraman Palmer, Michelle Whitesell, Luke Lindquist, Susan Schreiber, Stuart L Munoz, Benito Beilstein J Org Chem Full Research Paper The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure–activity relationships led to the discovery of ML212. Beilstein-Institut 2013-07-26 /pmc/articles/PMC3740683/ /pubmed/23946849 http://dx.doi.org/10.3762/bjoc.9.171 Text en Copyright © 2013, Youngsaye et al. https://creativecommons.org/licenses/by/2.0https://www.beilstein-journals.org/bjoc/termsThis is an Open Access article under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The license is subject to the Beilstein Journal of Organic Chemistry terms and conditions: (https://www.beilstein-journals.org/bjoc/terms)
spellingShingle Full Research Paper
Youngsaye, Willmen
Hartland, Cathy L
Morgan, Barbara J
Ting, Amal
Nag, Partha P
Vincent, Benjamin
Mosher, Carrie A
Bittker, Joshua A
Dandapani, Sivaraman
Palmer, Michelle
Whitesell, Luke
Lindquist, Susan
Schreiber, Stuart L
Munoz, Benito
ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
title ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
title_full ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
title_fullStr ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
title_full_unstemmed ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
title_short ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
title_sort ml212: a small-molecule probe for investigating fluconazole resistance mechanisms in candida albicans
topic Full Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3740683/
https://www.ncbi.nlm.nih.gov/pubmed/23946849
http://dx.doi.org/10.3762/bjoc.9.171
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