Cargando…
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...
Autores principales: | , , , , , , , , , , , , , |
---|---|
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 |
_version_ | 1782280172642238464 |
---|---|
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. |
format | Online Article Text |
id | pubmed-3740683 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Beilstein-Institut |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT youngsayewillmen ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT hartlandcathyl ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT morganbarbaraj ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT tingamal ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT nagparthap ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT vincentbenjamin ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT moshercarriea ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT bittkerjoshuaa ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT dandapanisivaraman ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT palmermichelle ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT whitesellluke ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT lindquistsusan ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT schreiberstuartl ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans AT munozbenito ml212asmallmoleculeprobeforinvestigatingfluconazoleresistancemechanismsincandidaalbicans |