ArticleThe Journal of infectious diseases2013
A novel calcium-dependent protein kinase inhibitor as a lead compound for treating cryptosporidiosis.
Article in The Journal of infectious diseases, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers.
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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.
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Who cites it
57 citing papers in PubMed, 77 citations in OpenAlex.
- Integrated Phytochemical, Computational and In Vitro Evaluation of the Oocysticidal Activity of Pleurotus ostreatus Extract Against Cryptosporidium parvum.Cell biochemistry and biophysics · 2026Article
- Norditerpene Natural Products from Subterranean Fungi with Anti-Parasitic Activity.Microorganisms · 2025Article
- Molecular pathogenesis of Cryptosporidium and advancements in therapeutic interventions.Parasite (Paris, France) · 2025Review
- Pyridopyrimidinones as a new chemotype of calcium dependent protein kinase 1 (CDPK1) inhibitors for Cryptosporidium.Molecular and biochemical parasitology · 2024Article
- Identification of potent and orally efficacious phosphodiesterase inhibitors in Cryptosporidium parvum-infected immunocompromised male mice.Nature communications · 2024Article
- Anti-Cryptosporidial Drug-Discovery Challenges and Existing Therapeutic Avenues: A "One-Health" Concern.Life (Basel, Switzerland) · 2024Review
- Understanding theFrontiers in parasitology · 2024Review
- Structure-activity relationship of BMS906024 derivatives for Cryptosporidium parvum growth inhibition.Bioorganic & medicinal chemistry letters · 2023Article
- A case of septic shock due to delayed diagnosis of Cryptosporidium infection after liver transplantation.BMC infectious diseases · 2023Article
- On-target inhibition of Cryptosporidium parvum by nitazoxanide (NTZ) and paclitaxel (PTX) validated using a novel MDR1-transgenic host cell model and algorithms to quantify the effect on the parasite target.PLoS neglected tropical diseases · 2023Article
- High-Throughput Screening of a Marine Compound Library Identifies Anti-Marine drugs · 2022Article
- Endochin-like quinolones (ELQs) and bumped kinase inhibitors (BKIs): Synergistic and additive effects of combined treatments against Neospora caninum infection in vitro and in vivo.International journal for parasitology. Drugs and drug resistance · 2021Article
- Systemic efficacy onParasitology · 2021Article
- Pyrrolopyrimidine Bumped Kinase Inhibitors for the Treatment of Cryptosporidiosis.ACS infectious diseases · 2021Article
- Bicyclic azetidines kill the diarrheal pathogenScience translational medicine · 2020Article
- A Conditional Protein Degradation System To Study Essential Gene Function in Cryptosporidium parvum.mBio · 2020Article
- Identification of a potent benzoxaborole drug candidate for treating cryptosporidiosis.Nature communications · 2019Article
- A suite of phenotypic assays to ensure pipeline diversity when prioritizing drug-like Cryptosporidium growth inhibitors.Nature communications · 2019Article
- Development of 5-Aminopyrazole-4-carboxamide-based Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.Journal of medicinal chemistry · 2019Article
- Discovery of Novel Anti-cryptosporidial Activities From Natural Products byFrontiers in microbiology · 2019Article
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
Abstract
Cryptosporidium parasites infect intestinal cells, causing cryptosporidiosis. Despite its high morbidity and association with stunting in the developing world, current therapies for cryptosporidiosis have limited efficacy. Calcium-dependent protein kinases (CDPKs) are essential enzymes in the biology of protozoan parasites. CDPK1 was cloned from the genome of Cryptosporidium parvum, and potent and specific inhibitors have been developed based on structural studies. In this study, we evaluated the anti-Cryptosporidium activity of a novel CDPK1 inhibitor, 1294, and demonstrated that 1294 significantly reduces parasite infection in vitro, with a half maximal effective concentration of 100 nM. Pharmacokinetic studies revealed that 1294 is well absorbed, with a half-life supporting daily administration. Oral therapy with 1294 eliminated Cryptosporidium parasites from 6 of 7 infected severe combined immunodeficiency-beige mice, and the parasites did not recur in these immunosuppressed mice. Mice treated with 1294 had less epithelial damage, corresponding to less apoptosis. Thus, 1294 is an important lead for the development of drugs for treatment of cryptosporidiosis.
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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.