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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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5659129/
https://www.ncbi.nlm.nih.gov/pubmed/28815830
http://dx.doi.org/10.1002/anie.201707324

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