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Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase.
Vinayak, Sumiti; Jumani, Rajiv S; Miller, Peter; Hasan, Muhammad M; McLeod, Briana I; Tandel, Jayesh; Stebbins, Erin E; Teixeira, Jose E; Borrel, Julien; Gonse, Arthur; Zhang, Mingliang; Yu, Xianshui; Wernimont, Amy; Walpole, Chris; Eckley, Sean; Love, Melissa S; McNamara, Case W; Sharma, Manmohan; Sharma, Amit; Scherer, Christina A; Kato, Nobutaka; Schreiber, Stuart L; Melillo, Bruno; Striepen, Boris; Huston, Christopher D; Comer, Eamon.
Affiliation
  • Vinayak S; Department of Pathobiology, College of Veterinary Medicine, University of Illinois at Urbana-Champaign, Urbana, IL 61802, USA.
  • Jumani RS; Cellular, Molecular and Biomedical Sciences Graduate Program, University of Vermont, Burlington, VT 05405, USA.
  • Miller P; Department of Medicine, Larner College of Medicine, University of Vermont, Burlington, VT 05405, USA.
  • Hasan MM; Cellular, Molecular and Biomedical Sciences Graduate Program, University of Vermont, Burlington, VT 05405, USA.
  • McLeod BI; Department of Pathobiology, School of Veterinary Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
  • Tandel J; Department of Pathobiology, School of Veterinary Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
  • Stebbins EE; Department of Medicine, Larner College of Medicine, University of Vermont, Burlington, VT 05405, USA.
  • Teixeira JE; Department of Medicine, Larner College of Medicine, University of Vermont, Burlington, VT 05405, USA.
  • Borrel J; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.
  • Gonse A; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.
  • Zhang M; International Discovery Service Unit, WuXi AppTec (Tianjin) Co. Ltd., Tianjin 300457, P.R. China.
  • Yu X; International Discovery Service Unit, WuXi AppTec (Tianjin) Co. Ltd., Tianjin 300457, P.R. China.
  • Wernimont A; Structural Genomics Consortium, MaRS Building, South Tower, 101 College Street, Suite 700, Toronto, Ontario M5G 1L7, Canada.
  • Walpole C; Structural Genomics Consortium, MaRS Building, South Tower, 101 College Street, Suite 700, Toronto, Ontario M5G 1L7, Canada.
  • Eckley S; Eisai Inc., Cambridge, MA 02140, USA.
  • Love MS; Calibr, a division of The Scripps Research Institute, La Jolla, CA 92037, USA.
  • McNamara CW; Calibr, a division of The Scripps Research Institute, La Jolla, CA 92037, USA.
  • Sharma M; Structural Parasitology, Molecular Medicine Group, International Centre for Genetic Engineering and Biotechnology, Aruna Asaf Ali Road, New Delhi 110070, India.
  • Sharma A; Structural Parasitology, Molecular Medicine Group, International Centre for Genetic Engineering and Biotechnology, Aruna Asaf Ali Road, New Delhi 110070, India.
  • Scherer CA; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.
  • Kato N; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.
  • Schreiber SL; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.
  • Melillo B; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
  • Striepen B; Chemical Biology and Therapeutics Science Program, Broad Institute, Cambridge, MA 02142, USA.
  • Huston CD; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
  • Comer E; Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
Sci Transl Med ; 12(563)2020 09 30.
Article in En | MEDLINE | ID: mdl-32998973
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Full text: 1 Database: MEDLINE Main subject: Parasites / Phenylalanine-tRNA Ligase / Azetidines / Cryptosporidiosis / Cryptosporidium Limits: Animals Language: En Journal: Sci Transl Med Journal subject: CIENCIA / MEDICINA Year: 2020 Type: Article Affiliation country: United States
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Full text: 1 Database: MEDLINE Main subject: Parasites / Phenylalanine-tRNA Ligase / Azetidines / Cryptosporidiosis / Cryptosporidium Limits: Animals Language: En Journal: Sci Transl Med Journal subject: CIENCIA / MEDICINA Year: 2020 Type: Article Affiliation country: United States