Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase
| Autor: | Sumiti Vinayak, Amy K. Wernimont, Chris Walpole, Sean Eckley, Jose E. Teixeira, Rajiv S. Jumani, Amit Sharma, Manmohan Sharma, Xianshui Yu, Christina Scherer, Nobutaka Kato, Muhammad M. Hasan, Bruno Melillo, Arthur Gonse, Christopher D. Huston, Stuart L. Schreiber, Eamon Comer, Boris Striepen, Case W. McNamara, Erin E. Stebbins, Briana I. McLeod, Julien Borrel, Jayesh Tandel, Melissa S. Love, Peter J. Miller, Mingliang Zhang |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
biology Bicyclic molecule 030106 microbiology Cryptosporidium General Medicine biology.organism_classification In vitro Microbiology 03 medical and health sciences Drug repositioning 030104 developmental biology Cryptosporidium parvum parasitic diseases Parasite hosting Pathogen EC50 |
| Zdroj: | Science Translational Medicine. 12 |
| ISSN: | 1946-6242 1946-6234 |
| DOI: | 10.1126/scitranslmed.aba8412 |
| Popis: | Cryptosporidium is a protozoan parasite and a leading cause of diarrheal disease and mortality in young children. Currently, there are no fully effective treatments available to cure infection with this diarrheal pathogen. In this study, we report a broad drug repositioning effort that led to the identification of bicyclic azetidines as a new anticryptosporidial series. Members of this series blocked growth in in vitro culture of three Cryptosporidium parvum isolates with EC50’s in 1% serum of |
| Databáze: | OpenAIRE |
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