Article

Selectivity of the time-dependent <i>M. tuberculosis</i> LeuRS inhibitor ganfeborole is driven by target vulnerability

2025-08-03

Abstract excerpt

<h4>ABSTRACT</h4> Ganfeborole (GSK3036656) inhibits the Mycobacterium tuberculosis leucyl-tRNA-synthetase (mtLeuRS) and is in phase 2a clinical trials for the treatment of tuberculosis. Here we show that ganfeborole is a time-dependent inhibitor of mtLeuRS (IC 50 1 nM) and generates a post-antibiotic effect of 77 h at 50xMIC (MIC 0.058 μM) with M. tuberculosis H37Rv ( Mtb ), indicating that mtLeuRS is a highl...

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Literature Corpus work: c02f376e-97a9-5745-bded-5fa7684778b1
DOI: 10.1101/2025.07.31.667927

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