Epidrugs as Promising Tools to Eliminate <i>Plasmodium falciparum</i> Artemisinin-Resistant and Quiescent Parasites
The use of artemisinin and its derivatives has helped reduce the burden of malaria caused by <i>Plasmodium falciparum.</i> However, artemisinin-resistant parasites are able, in the presence of artemisinins, to stop their cell cycles. This quiescent state can alter the activity of artemis...
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2023-10-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_e04148a7b56b4e0794e981d27ef6714e | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Thibaud Reyser |e author |
| 700 | 1 | 0 | |a Lucie Paloque |e author |
| 700 | 1 | 0 | |a Michel Nguyen |e author |
| 700 | 1 | 0 | |a Jean-Michel Augereau |e author |
| 700 | 1 | 0 | |a Matthew John Fuchter |e author |
| 700 | 1 | 0 | |a Marie Lopez |e author |
| 700 | 1 | 0 | |a Paola B. Arimondo |e author |
| 700 | 1 | 0 | |a Storm Hassell-Hart |e author |
| 700 | 1 | 0 | |a John Spencer |e author |
| 700 | 1 | 0 | |a Luisa Di Stefano |e author |
| 700 | 1 | 0 | |a Françoise Benoit-Vical |e author |
| 245 | 0 | 0 | |a Epidrugs as Promising Tools to Eliminate <i>Plasmodium falciparum</i> Artemisinin-Resistant and Quiescent Parasites |
| 260 | |b MDPI AG, |c 2023-10-01T00:00:00Z. | ||
| 500 | |a 10.3390/pharmaceutics15102440 | ||
| 500 | |a 1999-4923 | ||
| 520 | |a The use of artemisinin and its derivatives has helped reduce the burden of malaria caused by <i>Plasmodium falciparum.</i> However, artemisinin-resistant parasites are able, in the presence of artemisinins, to stop their cell cycles. This quiescent state can alter the activity of artemisinin partner drugs leading to a secondary drug resistance and thus threatens malaria eradication strategies. Drugs targeting epigenetic mechanisms (namely epidrugs) are emerging as potential antimalarial drugs. Here, we set out to evaluate a selection of various epidrugs for their activity against quiescent parasites, to explore the possibility of using these compounds to counter artemisinin resistance. The 32 chosen epidrugs were first screened for their antiplasmodial activity and selectivity. We then demonstrated, thanks to the specific Quiescent-stage Survival Assay, that four epidrugs targeting both histone methylation or deacetylation as well as DNA methylation decrease the ability of artemisinin-resistant parasites to recover after artemisinin exposure. In the quest for novel antiplasmodial drugs with new modes of action, these results reinforce the therapeutic potential of epidrugs as antiplasmodial drugs especially in the context of artemisinin resistance. | ||
| 546 | |a EN | ||
| 690 | |a malaria | ||
| 690 | |a epigenetics | ||
| 690 | |a artemisinin resistance | ||
| 690 | |a quiescent parasites | ||
| 690 | |a epidrugs | ||
| 690 | |a Pharmacy and materia medica | ||
| 690 | |a RS1-441 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Pharmaceutics, Vol 15, Iss 10, p 2440 (2023) | |
| 787 | 0 | |n https://www.mdpi.com/1999-4923/15/10/2440 | |
| 787 | 0 | |n https://doaj.org/toc/1999-4923 | |
| 856 | 4 | 1 | |u https://doaj.org/article/e04148a7b56b4e0794e981d27ef6714e |z Connect to this object online. |