ArticlePLoS pathogens2022
Inhibitors of ApiAP2 protein DNA binding exhibit multistage activity against Plasmodium parasites.
Article in PLoS pathogens, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 30 citations in OpenAlex.
- Targeting protein-protein interactions in Plasmodium: from asexual replication to sexual development.Parasites & vectors · 2026Review
- Chromatin state dynamics during the Plasmodium falciparum intraerythrocytic development cycle.BMC genomics · 2026Article
- Mining of Novkitasetaline, a New Sulfur-Containing Antimalarial β-Carboline Alkaloid, fromMicroorganisms · 2025Article
- Structural characterization of the ACDC domain from ApiAP2 proteins, a potential molecular target against apicomplexan parasites.Acta crystallographica. Section D, Structural biology · 2025Article
- Low nucleotide diversity of the Plasmodium falciparum AP2-EXP2 gene among clinical samples from Ghana.Parasites & vectors · 2024Article
- Unraveling the complexities of ApiAP2 regulation in Plasmodium falciparum.Trends in parasitology · 2024Review
- AeLife · 2024Article
- DNA sequence and chromatin differentiate sequence-specific transcription factor binding in the human malaria parasite Plasmodium falciparum.Nucleic acids research · 2024Article
- Identification and function characterization of NcAP2XII-4 in Neospora caninum.Parasites & vectors · 2024Article
- Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum.Malaria journal · 2024Review
- Review
- Histone modification analysis reveals common regulators of gene expression in liver and blood stage merozoites of Plasmodium parasites.Epigenetics & chromatin · 2023Article
- Toxoplasma gondii AP2XII-2 Contributes to Transcriptional Repression for Sexual Commitment.mSphere · 2023Article
- Long-Read Genome Assembly and Gene Model Annotations for the Rodent Malaria ParasitebioRxiv : the preprint server for biology · 2023Article
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Authors and funding
14 authors at 7 institutions in 5 countries.
Funding
Abstract
Plasmodium parasites are reliant on the Apicomplexan AP2 (ApiAP2) transcription factor family to regulate gene expression programs. AP2 DNA binding domains have no homologs in the human or mosquito host genomes, making them potential antimalarial drug targets. Using an in-silico screen to dock thousands of small molecules into the crystal structure of the AP2-EXP (Pf3D7_1466400) AP2 domain (PDB:3IGM), we identified putative AP2-EXP interacting compounds. Four compounds were found to block DNA binding by AP2-EXP and at least one additional ApiAP2 protein. Our top ApiAP2 competitor compound perturbs the transcriptome of P. falciparum trophozoites and results in a decrease in abundance of log2 fold change > 2 for 50% (46/93) of AP2-EXP target genes. Additionally, two ApiAP2 competitor compounds have multi-stage anti-Plasmodium activity against blood and mosquito stage parasites. In summary, we describe a novel set of antimalarial compounds that interact with AP2 DNA binding domains. These compounds may be used for future chemical genetic interrogation of ApiAP2 proteins or serve as starting points for a new class of antimalarial therapeutics.
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Registered trials
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