ArticleCell discovery2020
A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1.
Article in Cell discovery, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed, 54 citations in OpenAlex.
- Hydroxamic Acids as HDAC Inhibitor Drug Leads for Malaria.Medicinal research reviews · 2026Review
- Repurposing 6‑Anilinopurine Derivatives That Exhibit PfHDAC1 Inhibition and Antimalarial Activity against Asexual and Sexual Stages ofACS omega · 2026Article
- Paclitaxel-induced tubulin dysfunction stalls parasite development: synergistic potential with artemisinin against resistant strains.Microbiology spectrum · 2026Article
- Importance of the inflammasome in gut-brain axis: from pathological driver to therapeutic target.Inflammopharmacology · 2026Review
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- Article
- Marine Guanidine Alkaloids Inhibit Malaria Parasites Development inACS infectious diseases · 2025Article
- β-hydroxybutyrate inhibits Plasmodium falciparum development and confers protection against malaria in mice.Nature metabolism · 2025Article
- Antimalarial Drug Discovery from Natural and Synthetic Sources.Current medicinal chemistry · 2025Review
- Onametostat, a PfPRMT5 inhibitor, exhibits antimalarial activity toAntimicrobial agents and chemotherapy · 2024Article
- Innovative Multistage ML-QSAR Models for Malaria: From Data to Discovery.ACS medicinal chemistry letters · 2024Article
- Transmission-Blocking Strategies for Malaria Eradication: Recent Advances in Small-Molecule Drug Development.Pharmaceuticals (Basel, Switzerland) · 2024Review
- PfHDAC1 is an essential regulator ofmBio · 2024Article
- Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum.Malaria journal · 2024Review
- 1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors.Scientific reports · 2023Article
- Harnessing the cyclization strategy for new drug discovery.Acta pharmaceutica Sinica. B · 2022Review
- Cucurbitacin B-induced G2/M cell cycle arrest of conjunctival melanoma cells mediated by GRP78-FOXM1-KIF20A pathway.Acta pharmaceutica Sinica. B · 2022Article
- A heme-activatable probe and its application in the high-throughput screening of Plasmodium falciparum ring-stage inhibitors.Signal transduction and targeted therapy · 2022Article
- Combined Transcriptome and Proteome Profiling for Role of pfEMP1 in Antimalarial Mechanism of Action of Dihydroartemisinin.Microbiology spectrum · 2021Article
- Ten-Year Molecular Surveillance of Drug-ResistantFrontiers in cellular and infection microbiology · 2021Article
Corrections and comments
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Authors and funding
29 authors at 7 institutions in 2 countries.
Funding
Abstract
Although artemisinin combination therapies have succeeded in reducing the global burden of malaria, multidrug resistance of the deadliest malaria parasite, Plasmodium falciparum, is emerging worldwide. Innovative antimalarial drugs that kill all life-cycle stages of malaria parasites are urgently needed. Here, we report the discovery of the compound JX21108 with broad antiplasmodial activity against multiple life-cycle stages of malaria parasites. JX21108 was developed from chemical optimization of quisinostat, a histone deacetylase inhibitor. We identified P. falciparum histone deacetylase 1 (PfHDAC1), an epigenetic regulator essential for parasite growth and invasion, as a molecular target of JX21108. PfHDAC1 knockdown leads to the downregulation of essential parasite genes, which is highly consistent with the transcriptomic changes induced by JX21108 treatment. Collectively, our data support that PfHDAC1 is a potential drug target for overcoming multidrug resistance and that JX21108 treats malaria and blocks parasite transmission simultaneously.
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.