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Antifungal Drugs
We reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-β-d-glucan synthase, lanosterol 14-α-demethylase, protein, and deoxyribonucleic acid biosynthesis, or sequestrate erg...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7143493/ https://www.ncbi.nlm.nih.gov/pubmed/32178468 http://dx.doi.org/10.3390/metabo10030106 |
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author | Houšť, Jiří Spížek, Jaroslav Havlíček, Vladimír |
author_facet | Houšť, Jiří Spížek, Jaroslav Havlíček, Vladimír |
author_sort | Houšť, Jiří |
collection | PubMed |
description | We reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-β-d-glucan synthase, lanosterol 14-α-demethylase, protein, and deoxyribonucleic acid biosynthesis, or sequestrate ergosterol. Their most severe side effects are hepatotoxicity, nephrotoxicity, and myelotoxicity. Whereas triazoles exhibit the most significant drug–drug interactions, echinocandins exhibit almost none. The antifungal resistance may be developed across most pathogens and includes drug target overexpression, efflux pump activation, and amino acid substitution. The experimental antifungal drugs in clinical trials are also reviewed. Siderophores in the Trojan horse approach or the application of siderophore biosynthesis enzyme inhibitors represent the most promising emerging antifungal therapies. |
format | Online Article Text |
id | pubmed-7143493 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-71434932020-04-14 Antifungal Drugs Houšť, Jiří Spížek, Jaroslav Havlíček, Vladimír Metabolites Review We reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-β-d-glucan synthase, lanosterol 14-α-demethylase, protein, and deoxyribonucleic acid biosynthesis, or sequestrate ergosterol. Their most severe side effects are hepatotoxicity, nephrotoxicity, and myelotoxicity. Whereas triazoles exhibit the most significant drug–drug interactions, echinocandins exhibit almost none. The antifungal resistance may be developed across most pathogens and includes drug target overexpression, efflux pump activation, and amino acid substitution. The experimental antifungal drugs in clinical trials are also reviewed. Siderophores in the Trojan horse approach or the application of siderophore biosynthesis enzyme inhibitors represent the most promising emerging antifungal therapies. MDPI 2020-03-12 /pmc/articles/PMC7143493/ /pubmed/32178468 http://dx.doi.org/10.3390/metabo10030106 Text en © 2020 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 | Review Houšť, Jiří Spížek, Jaroslav Havlíček, Vladimír Antifungal Drugs |
title | Antifungal Drugs |
title_full | Antifungal Drugs |
title_fullStr | Antifungal Drugs |
title_full_unstemmed | Antifungal Drugs |
title_short | Antifungal Drugs |
title_sort | antifungal drugs |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7143493/ https://www.ncbi.nlm.nih.gov/pubmed/32178468 http://dx.doi.org/10.3390/metabo10030106 |
work_keys_str_mv | AT houstjiri antifungaldrugs AT spizekjaroslav antifungaldrugs AT havlicekvladimir antifungaldrugs |