The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
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37<br />
<strong>GSK2251052</strong>: Pre-Cl<strong>in</strong>ical Mechanism<br />
<strong>of</strong> Resistance<br />
Laboratory generated mutants resistant to <strong>GSK2251052</strong> conta<strong>in</strong> mutations<br />
<strong>in</strong> the LeuRS edit<strong>in</strong>g doma<strong>in</strong><br />
– S<strong>in</strong>gle-step mutations <strong>in</strong> leuS<br />
<strong>GSK2251052</strong> MICs <strong>of</strong> resistant mutants range from 32->256 mcg/mL<br />
Organism<br />
<strong>GSK2251052</strong> MIC (mcg/ml)<br />
WT<br />
Mutants<br />
E. coli 1 64‐>256<br />
K. pneumoniae 1 256‐>256<br />
P. aerug<strong>in</strong>osa 4 32‐>256<br />
– <strong>GSK2251052</strong> resistant mutants do not confer cross-resistance to other<br />
antibiotics and appear to be edit<strong>in</strong>g deficient
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