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Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against Trypanosoma brucei

Based on crystal structures of Trypanosoma brucei methionyl-tRNA synthetase (TbMetRS) bound to inhibitors, we designed, synthesized, and evaluated two series of novel TbMetRS inhibitors targeting this parasite enzyme. One series has a 1,3-dihydro-imidazol-2-one containing linker, the other has a rig...

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Détails bibliographiques
Publié dans:RSC Med Chem
Auteurs principaux: Zhang, Zhongsheng, Barros-Álvarez, Ximena, Gillespie, J. Robert, Ranade, Ranae M., Huang, Wenlin, Shibata, Sayaka, Molasky, Nora M. R., Faghih, Omeed, Mushtaq, Aisha, Choy, Robert K. M., de Hostos, Eugenio, Hol, Wim G. J., Verlinde, Christophe L. M. J., Buckner, Frederick S., Fan, Erkang
Format: Artigo
Langue:Inglês
Publié: Royal Society of Chemistry 2020
Sujets:
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC7649832/
https://ncbi.nlm.nih.gov/pubmed/33479683
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/d0md00057d
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