Drug design from the cryptic inhibitor envelope
@article{Lee2016DrugDF, title={Drug design from the cryptic inhibitor envelope}, author={C. Lee and Xiaofei Liang and Qinglin Wu and Javaria Najeeb and Jinshi Zhao and Ramesh Gopalaswamy and M. Tit{\'e}cat and F. Sebbane and N. Lema{\^i}tre and E. Toone and P. Zhou}, journal={Nature Communications}, year={2016}, volume={7} }
Conformational dynamics plays an important role in enzyme catalysis, allosteric regulation of protein functions and assembly of macromolecular complexes. Despite these well-established roles, such information has yet to be exploited for drug design. Here we show by nuclear magnetic resonance spectroscopy that inhibitors of LpxC—an essential enzyme of the lipid A biosynthetic pathway in Gram-negative bacteria and a validated novel antibiotic target—access alternative, minor population states in… Expand
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