ArticleAntimicrobial agents and chemotherapy2013
Broad-spectrum antimalarial activity of peptido sulfonyl fluorides, a new class of proteasome inhibitors.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
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Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Ubiquitin-proteasome system inFrontiers in medicine · 2024Pooled it
- Organocatalytic Enantioselective Addition of 3-Aryloxindoles to Ethenesulfonyl Fluoride.Organic letters · 2025Article
- Combating Malaria: Targeting the Ubiquitin-Proteasome System to Conquer Drug Resistance.Tropical medicine and infectious disease · 2025Review
- Structural comparison of human and Plasmodium proteasome β5 subunits: informing selective inhibitor design for anti-malaria agents.Malaria journal · 2025Article
- Vaginal Tritrichomonas foetus infection in mice as an in vivo model for drug development against Trichomonas vaginalis.PloS one · 2024Article
- Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome.Cell chemical biology · 2023Article
- Epoxomicin, a Selective Proteasome Inhibitor, Activates AIM2 Inflammasome in Human Retinal Pigment Epithelium Cells.Antioxidants (Basel, Switzerland) · 2022Article
- Targeting Proteasomes in Cancer and Infectious Disease: A Parallel Strategy to Treat Malignancies and Microbes.Frontiers in cellular and infection microbiology · 2022Review
- Microbial proteasomes as drug targets.PLoS pathogens · 2021Review
- Design of proteasome inhibitors with oral efficacy in vivo againstProceedings of the National Academy of Sciences of the United States of America · 2021Article
- Article
- Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.Journal of medicinal chemistry · 2018Article
- The proteasome as a target to combat malaria: hits and misses.Translational research : the journal of laboratory and clinical medicine · 2018Review
- Using Yeast Synthetic Lethality To Inform Drug Combination for Malaria.Antimicrobial agents and chemotherapy · 2018Article
- Protein Degradation Systems as Antimalarial Therapeutic Targets.Trends in parasitology · 2017Review
- Artemisinin Action and Resistance in Plasmodium falciparum.Trends in parasitology · 2016Review
- Sulfonyl fluorides as privileged warheads in chemical biology.Chemical science · 2015Article
- Targeting the cell stress response of Plasmodium falciparum to overcome artemisinin resistance.PLoS biology · 2015Article
- Profound activity of the anti-cancer drug bortezomib against Echinococcus multilocularis metacestodes identifies the proteasome as a novel drug target for cestodes.PLoS neglected tropical diseases · 2014Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Despite declining numbers of cases and deaths, malaria remains a major public health problem in many parts of the world. Today, case management relies heavily on a single class of antimalarial compounds: artemisinins. Hence, development of resistance against artemisinins may destroy current malaria control strategies. Beyond malaria control are elimination and eradication programs that will require drugs with good activity against acute infection but also with preventive and transmission-blocking properties. Consequently, new antimalarials are needed not only to ensure malaria control but also for elimination and eradication efforts. In this study, we introduce peptido sulfonyl fluorides (PSF) as a new class of compounds with antiplasmodial activity. We show that PSF target the plasmodial proteasome and act on all asexual stages of the intraerythrocytic cycle and on gametocytes. PSF showed activities at concentrations as low as 20 nM against multidrug-resistant and chloroquine-sensitive Plasmodium falciparum laboratory strains and clinical isolates from Gabon. Structural requirements for activity were identified, and cytotoxicity in human HeLa or HEK 293 cells was low. The lead PSF PW28 suppressed growth of Plasmodium berghei in vivo but showed signs of toxicity in mice. Considering their modular structure and broad spectrum of activity against different stages of the plasmodial life cycle, proteasome inhibitors based on PSF have a great potential for further development as preclinical candidate compounds with improved species-specific activity and less toxicity.
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