National Institutes of Health/National Institute Of Allergy and Infectious Diseases (NIH/NIAID)
R33AI127635
United States
Citation
Journal: Nat Commun / Year: 2023 Title: Non-covalent inhibitors of thioredoxin glutathione reductase with schistosomicidal activity in vivo. Authors: Valentina Z Petukhova / Sammy Y Aboagye / Matteo Ardini / Rachel P Lullo / Francesca Fata / Margaret E Byrne / Federica Gabriele / Lucy M Martin / Luke N M Harding / Vamshikrishna Gone / ...Authors: Valentina Z Petukhova / Sammy Y Aboagye / Matteo Ardini / Rachel P Lullo / Francesca Fata / Margaret E Byrne / Federica Gabriele / Lucy M Martin / Luke N M Harding / Vamshikrishna Gone / Bikash Dangi / Daniel D Lantvit / Dejan Nikolic / Rodolfo Ippoliti / Grégory Effantin / Wai Li Ling / Jeremy J Johnson / Gregory R J Thatcher / Francesco Angelucci / David L Williams / Pavel A Petukhov / Abstract: Only praziquantel is available for treating schistosomiasis, a disease affecting more than 200 million people. Praziquantel-resistant worms have been selected for in the lab and low cure rates from ...Only praziquantel is available for treating schistosomiasis, a disease affecting more than 200 million people. Praziquantel-resistant worms have been selected for in the lab and low cure rates from mass drug administration programs suggest that resistance is evolving in the field. Thioredoxin glutathione reductase (TGR) is essential for schistosome survival and a validated drug target. TGR inhibitors identified to date are irreversible and/or covalent inhibitors with unacceptable off-target effects. In this work, we identify noncovalent TGR inhibitors with efficacy against schistosome infections in mice, meeting the criteria for lead progression indicated by WHO. Comparisons with previous in vivo studies with praziquantel suggests that these inhibitors outperform the drug of choice for schistosomiasis against juvenile worms.
Film or detector model: GATAN K2 SUMMIT (4k x 4k) / Digitization - Frames/image: 1-50 / Number grids imaged: 1 / Number real images: 2600 / Average electron dose: 50.0 e/Å2
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