Optimization of a binding fragment targeting the “enlarged methionine pocket” leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors

Potent inhibitors of Trypanosoma brucei methionyl-tRNA synthetase were previously designed using a structure-guided approach. Compounds 1 and 2 were the most active compounds in the cyclic and linear linker series, respectively. To further improve cellular potency, SAR investigation of a binding fra...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Huang, Wenlin, Zhang, Zhongsheng, Ranade, Ranae M., Gillespie, J. Robert, Barros-Álvarez, Ximena, Creason, Sharon A., Shibata, Sayaka, Verlinde, Christophe L. M. J., Hol, Wim G. J., Buckner, Frederick S., Fan, Erkang
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5542777/
https://ncbi.nlm.nih.gov/pubmed/28465105
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.04.048
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