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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Tallennettuna:
Bibliografiset tiedot
Julkaisussa:Angew Chem Int Ed Engl
Päätekijät: 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
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: John Wiley and Sons Inc. 2017
Aiheet:
Communications
Linkit: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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