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...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2022-12-01
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| Series: | International Journal for Parasitology: Drugs and Drug Resistance |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211320722000288 |
| _version_ | 1811295600599105536 |
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| author | Matthew P. Challis Shane M. Devine Darren J. Creek |
| author_facet | Matthew P. Challis Shane M. Devine Darren J. Creek |
| author_sort | Matthew P. Challis |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-04-13T05:35:50Z |
| format | Article |
| id | doaj.art-80c228a22fa7455bb8385efef7f26dce |
| institution | Directory Open Access Journal |
| issn | 2211-3207 |
| language | English |
| last_indexed | 2024-04-13T05:35:50Z |
| publishDate | 2022-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | International Journal for Parasitology: Drugs and Drug Resistance |
| spelling | doaj.art-80c228a22fa7455bb8385efef7f26dce2022-12-22T03:00:18ZengElsevierInternational Journal for Parasitology: Drugs and Drug Resistance2211-32072022-12-0120135144Current and emerging target identification methods for novel antimalarialsMatthew P. Challis0Shane M. Devine1Darren J. Creek2Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, AustraliaMedicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, AustraliaDrug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia; Corresponding author. Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, 3052, Australia.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.http://www.sciencedirect.com/science/article/pii/S2211320722000288Target identificationPlasmodium falciparumAntimalarialCETSAChemoproteomics |
| spellingShingle | Matthew P. Challis Shane M. Devine Darren J. Creek Current and emerging target identification methods for novel antimalarials International Journal for Parasitology: Drugs and Drug Resistance Target identification Plasmodium falciparum Antimalarial CETSA Chemoproteomics |
| 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 | Target identification Plasmodium falciparum Antimalarial CETSA Chemoproteomics |
| url | http://www.sciencedirect.com/science/article/pii/S2211320722000288 |
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