ArticleThe Journal of antimicrobial chemotherapy2012
Novel anti-Cryptosporidium activity of known drugs identified by high-throughput screening against parasite fatty acyl-CoA binding protein (ACBP).
Article in The Journal of antimicrobial chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 34 citations in OpenAlex.
- Broxyquinoline enhances antibacterial activity of colistin and attenuates LPS-induced inflammation.Antimicrobial agents and chemotherapy · 2026Article
- Anti-Cryptosporidial Drug-Discovery Challenges and Existing Therapeutic Avenues: A "One-Health" Concern.Life (Basel, Switzerland) · 2024Review
- Discovery of 8-Hydroxyquinoline as a Histamine Receptor 2 Blocker Scaffold.ACS synthetic biology · 2022Article
- Activity of (1-benzyl-4-triazolyl)-indole-2-carboxamides against Toxoplasma gondii and Cryptosporidium parvum.International journal for parasitology. Drugs and drug resistance · 2022Article
- Changes in the Microbiome ofMicroorganisms · 2020Article
- Functional characterization of acyl-CoA binding protein in Neospora caninum.Parasites & vectors · 2020Article
- Insight into the Molecular Interaction of Cloxyquin (5-chloro-8-hydroxyquinoline) with Bovine Serum Albumin: Biophysical Analysis and Computational Simulation.International journal of molecular sciences · 2019Article
- Comprehensive Characterization ofmBio · 2018Article
- Discovery of ebselen as an inhibitor of Cryptosporidium parvum glucose-6-phosphate isomerase (CpGPI) by high-throughput screening of existing drugs.International journal for parasitology. Drugs and drug resistance · 2018Article
- A high-throughput phenotypic screen identifies clofazimine as a potential treatment for cryptosporidiosis.PLoS neglected tropical diseases · 2017Article
- Association of NMT2 with the acyl-CoA carrier ACBD6 protects the N-myristoyltransferase reaction from palmitoyl-CoA.Journal of lipid research · 2016Article
- A Proposed Target Product Profile and Developmental Cascade for New Cryptosporidiosis Treatments.PLoS neglected tropical diseases · 2015Article
- Remodeling of host phosphatidylcholine by Chlamydia acyltransferase is regulated by acyl-CoA binding protein ACBD6 associated with lipid droplets.MicrobiologyOpen · 2015Article
- Cryptosporidium Lactate Dehydrogenase Is Associated with the Parasitophorous Vacuole Membrane and Is a Potential Target for Developing Therapeutics.PLoS pathogens · 2015Article
- A review of the global burden, novel diagnostics, therapeutics, and vaccine targets for cryptosporidium.The Lancet. Infectious diseases · 2015Review
- A unique hexokinase in Cryptosporidium parvum, an apicomplexan pathogen lacking the Krebs cycle and oxidative phosphorylation.Protist · 2014Article
- Amelioration of Cryptosporidium parvum infection in vitro and in vivo by targeting parasite fatty acyl-coenzyme A synthetases.The Journal of infectious diseases · 2014Article
- Validation of IMP dehydrogenase inhibitors in a mouse model of cryptosporidiosis.Antimicrobial agents and chemotherapy · 2014Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundCryptosporidium parvum causes an opportunistic infection in AIDS patients, and no effective treatments are yet available. This parasite possesses a single fatty acyl-CoA binding protein (CpACBP1) that is localized to the unique parasitophorous vacuole membrane (PVM). The major goal of this study was to identify inhibitors from known drugs against CpACBP1 as potential new anti-Cryptosporidium agents.
methodsA fluorescence assay was developed to detect CpACBP1 activity and to identify inhibitors by screening known drugs. Efficacies of top CpACBP1 inhibitors against Cryptosporidium growth in vitro were evaluated using a quantitative RT-PCR assay.
resultsNitrobenzoxadiazole-labelled palmitoyl-CoA significantly increased the fluorescent emission upon binding to CpACBP1 (excitation/emission 460/538 nm), which was quantified to determine the CpACBP1 activity and binding kinetics. The fluorescence assay was used to screen a collection of 1040 compounds containing mostly known drugs, and identified the 28 most active compounds that could inhibit CpACBP1 activity with sub-micromolar IC(50) values. Among them, four compounds displayed efficacies against parasite growth in vitro with low micromolar IC(50) values. The effective compounds were broxyquinoline (IC(50) 64.9 μM), cloxyquin (IC(50) 25.1 μM), cloxacillin sodium (IC(50) 36.2 μM) and sodium dehydrocholate (IC(50) 53.2 μM).
conclusionsThe fluorescence ACBP assay can be effectively used to screen known drugs or other compound libraries. Novel anti-Cryptosporidium activity was observed in four top CpACBP1 inhibitors, which may be further investigated for their potential to be repurposed to treat cryptosporidiosis and to serve as leads for drug development.
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