Determinants of the Inhibition of DprE1 and CYP2C9 by Antitubercular Thiophenes

Mycobacterium tuberculosis (Mtb) DprE1, an essential isomerase for the biosynthesis of the mycobacterial cell wall, is a validated target for tuberculosis (TB) drug development. Here we report the X‐ray crystal structures of DprE1 and the DprE1 resistant mutant (Y314C) in complexes with TCA1 derivat...

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Detalhes bibliográficos
Publicado no:Angew Chem Int Ed Engl
Main Authors: Liu, Renhe, Lyu, Xiaoxuan, Batt, Sarah M, Hsu, Mei‐Hui, Harbut, Michael B, Vilchèze, Catherine, Cheng, Bo, Ajayi, Kehinde, Yang, Baiyuan, Yang, Yun, Guo, Hui, Lin, Changyou, Gan, Fei, Wang, Chen, Franzblau, Scott G., Jacobs, William R., Besra, Gurdyal S., Johnson, Eric F., Petrassi, Mike, Chatterjee, Arnab K., Fütterer, Klaus, Wang, Feng
Formato: Artigo
Idioma:Inglês
Publicado em: John Wiley and Sons Inc. 2017
Assuntos:
Communications
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5659129/
https://ncbi.nlm.nih.gov/pubmed/28815830
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.201707324
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