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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Vydáno v:RSC Med Chem
Hlavní autoři: 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
Médium: Artigo
Jazyk:Inglês
Vydáno: Royal Society of Chemistry 2020
Témata:
Chemistry
On-line přístup: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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