ArticleChemistry & biology2010
Functional studies of Plasmodium falciparum dipeptidyl aminopeptidase I using small molecule inhibitors and active site probes.
Article in Chemistry & biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 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
37 citing papers in PubMed, 69 citations in OpenAlex.
- Structure-based discovery of Plasmodium falciparum DPAP-1 inhibitor and its experimental validation as an antimalarial agent.Folia microbiologica · 2026Article
- Therapeutic Targeting and Role of Cysteine Proteases in the Life Cycle of Malaria Parasite.Current medicinal chemistry · 2025Review
- Article
- A cathepsin C-like protease post-translationally modifiesbioRxiv : the preprint server for biology · 2023Article
- Two Tags in One Probe: Combining Fluorescence- and Biotin-based Detection of the Trypanosomal Cysteine Protease Rhodesain.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Targeting theHeliyon · 2022Review
- Review
- Chemoproteomics for Plasmodium Parasite Drug Target Discovery.Chembiochem : a European journal of chemical biology · 2021Review
- Methods Used to Investigate theFrontiers in cellular and infection microbiology · 2021Review
- System-wide biochemical analysis reveals ozonide antimalarials initially act by disrupting Plasmodium falciparum haemoglobin digestion.PLoS pathogens · 2020Article
- Article
- Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity identifies differences in amino acid preferences between peptide-based substrates and covalent inhibitors.The FEBS journal · 2019Article
- Clipped histone H3 is integrated into nucleosomes of DNA replication genes in the human malaria parasiteEMBO reports · 2019Article
- Identification of Plasmodium dipeptidyl aminopeptidase allosteric inhibitors by high throughput screening.PloS one · 2019Article
- Structural Insights Into KeyFrontiers in microbiology · 2019Review
- Proteases as antimalarial targets: strategies for genetic, chemical, and therapeutic validation.The FEBS journal · 2017Review
- Asymmetric synthesis of propargylamines as amino acid surrogates in peptidomimetics.Beilstein journal of organic chemistry · 2017Article
- Design and Synthesis of Activity-Based Probes and Inhibitors for Bleomycin Hydrolase.Chemistry & biology · 2015Article
- Drug delivery to the malaria parasite using an arterolane-like scaffold.ChemMedChem · 2015Article
- Identification, immunolocalization, and characterization analyses of an exopeptidase of papain superfamily, (cathepsin C) from Clonorchis sinensis.Parasitology research · 2014Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
The widespread resistance of malaria parasites to all affordable drugs has made the identification of new targets urgent. Dipeptidyl aminopeptidases (DPAPs) represent potentially valuable new targets that are involved in hemoglobin degradation (DPAP1) and parasite egress (DPAP3). Here we use activity-based probes to demonstrate that specific inhibition of DPAP1 by a small molecule results in the formation of an immature trophozoite that leads to parasite death. Using computational methods, we designed stable, nonpeptidic covalent inhibitors that kill Plasmodium falciparum at low nanomolar concentrations. These compounds show signs of slowing parasite growth in a murine model of malaria, which suggests that DPAP1 might be a viable antimalarial target. Interestingly, we found that resynthesis and activation of DPAP1 after inhibition is rapid, suggesting that effective drugs would need to sustain DPAP1 inhibition for a period of 2-3 hr.
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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.