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Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus
The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Sta...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5372984/ https://www.ncbi.nlm.nih.gov/pubmed/28134858 http://dx.doi.org/10.3390/antibiotics6010004 |
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author | Sweeney, Noreena L. Lipker, Lauren Hanson, Alicia M. Bohl, Chris J. Engel, Katie E. Kalous, Kelsey S. Stemper, Mary E. Sem, Daniel S. Schwan, William R. |
author_facet | Sweeney, Noreena L. Lipker, Lauren Hanson, Alicia M. Bohl, Chris J. Engel, Katie E. Kalous, Kelsey S. Stemper, Mary E. Sem, Daniel S. Schwan, William R. |
author_sort | Sweeney, Noreena L. |
collection | PubMed |
description | The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Staphylococcus aureus. Initially, the project was focused on discovering small molecules that may have antibacterial properties targeting the Mycobacterium tuberculosis thioredoxin reductase. This led to the discovery of a pyrazolone scaffold-containing compound series that showed bactericidal capability against S. aureus strains, including drug-resistant clinical isolates. The findings support continued development of the pyrazolone compounds as potential anti-S. aureus antibiotics. |
format | Online Article Text |
id | pubmed-5372984 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-53729842017-04-05 Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus Sweeney, Noreena L. Lipker, Lauren Hanson, Alicia M. Bohl, Chris J. Engel, Katie E. Kalous, Kelsey S. Stemper, Mary E. Sem, Daniel S. Schwan, William R. Antibiotics (Basel) Article The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Staphylococcus aureus. Initially, the project was focused on discovering small molecules that may have antibacterial properties targeting the Mycobacterium tuberculosis thioredoxin reductase. This led to the discovery of a pyrazolone scaffold-containing compound series that showed bactericidal capability against S. aureus strains, including drug-resistant clinical isolates. The findings support continued development of the pyrazolone compounds as potential anti-S. aureus antibiotics. MDPI 2017-01-28 /pmc/articles/PMC5372984/ /pubmed/28134858 http://dx.doi.org/10.3390/antibiotics6010004 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Sweeney, Noreena L. Lipker, Lauren Hanson, Alicia M. Bohl, Chris J. Engel, Katie E. Kalous, Kelsey S. Stemper, Mary E. Sem, Daniel S. Schwan, William R. Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus |
title | Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus |
title_full | Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus |
title_fullStr | Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus |
title_full_unstemmed | Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus |
title_short | Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus |
title_sort | docking into mycobacterium tuberculosis thioredoxin reductase protein yields pyrazolone lead molecules for methicillin-resistant staphylococcus aureus |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5372984/ https://www.ncbi.nlm.nih.gov/pubmed/28134858 http://dx.doi.org/10.3390/antibiotics6010004 |
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