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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...

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Detalles Bibliográficos
Autores principales: Challis, Matthew P., Devine, Shane M., Creek, Darren J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2022
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.
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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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