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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Dettagli Bibliografici
Pubblicato in:RSC Med Chem
Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: Royal Society of Chemistry 2020
Soggetti:
Chemistry
Accesso online: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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