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Determinants of the Inhibition of DprE1 and CYP2C9 by Antitubercular Thiophenes

17 Aug 2017

Abstract excerpt

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 derivatives to elucidate the molecular basis of their inhibitory activities and an unconventional resistance mechanism,...

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PMID: 28815830
DOI: 10.1002/anie.201707324

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