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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Publicat a:RSC Med Chem
Autors principals: 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
Idioma:Inglês
Publicat: Royal Society of Chemistry 2020
Matèries:
Chemistry
Accés en línia: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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