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Current and emerging target identification methods for novel antimalarials
New antimalarial compounds with novel mechanisms of action are urgently needed to combat the recent rise in antimalarial drug resistance. Phenotypic high-throughput screens have proven to be a successful method for identifying new compounds, however, do not provide mechanistic information about the...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9771836/ https://www.ncbi.nlm.nih.gov/pubmed/36410177 http://dx.doi.org/10.1016/j.ijpddr.2022.11.001 |
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author | Challis, Matthew P. Devine, Shane M. Creek, Darren J. |
author_facet | Challis, Matthew P. Devine, Shane M. Creek, Darren J. |
author_sort | Challis, Matthew P. |
collection | PubMed |
description | New antimalarial compounds with novel mechanisms of action are urgently needed to combat the recent rise in antimalarial drug resistance. Phenotypic high-throughput screens have proven to be a successful method for identifying new compounds, however, do not provide mechanistic information about the molecular target(s) responsible for antimalarial action. Current and emerging target identification methods such as in vitro resistance generation, metabolomics screening, chemoproteomic approaches and biophysical assays measuring protein stability across the whole proteome have successfully identified novel drug targets. This review provides an overview of these techniques, comparing their strengths and weaknesses and how they can be utilised for antimalarial target identification. |
format | Online Article Text |
id | pubmed-9771836 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-97718362022-12-23 Current and emerging target identification methods for novel antimalarials Challis, Matthew P. Devine, Shane M. Creek, Darren J. Int J Parasitol Drugs Drug Resist Review article New antimalarial compounds with novel mechanisms of action are urgently needed to combat the recent rise in antimalarial drug resistance. Phenotypic high-throughput screens have proven to be a successful method for identifying new compounds, however, do not provide mechanistic information about the molecular target(s) responsible for antimalarial action. Current and emerging target identification methods such as in vitro resistance generation, metabolomics screening, chemoproteomic approaches and biophysical assays measuring protein stability across the whole proteome have successfully identified novel drug targets. This review provides an overview of these techniques, comparing their strengths and weaknesses and how they can be utilised for antimalarial target identification. Elsevier 2022-11-11 /pmc/articles/PMC9771836/ /pubmed/36410177 http://dx.doi.org/10.1016/j.ijpddr.2022.11.001 Text en © 2022 The Authors https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Review article Challis, Matthew P. Devine, Shane M. Creek, Darren J. Current and emerging target identification methods for novel antimalarials |
title | Current and emerging target identification methods for novel antimalarials |
title_full | Current and emerging target identification methods for novel antimalarials |
title_fullStr | Current and emerging target identification methods for novel antimalarials |
title_full_unstemmed | Current and emerging target identification methods for novel antimalarials |
title_short | Current and emerging target identification methods for novel antimalarials |
title_sort | current and emerging target identification methods for novel antimalarials |
topic | Review article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9771836/ https://www.ncbi.nlm.nih.gov/pubmed/36410177 http://dx.doi.org/10.1016/j.ijpddr.2022.11.001 |
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