A unique small molecule inhibitor of enolase clarifies its role in fundamental biological processes.

@article{Jung2013AUS,
  title={A unique small molecule inhibitor of enolase clarifies its role in fundamental biological processes.},
  author={Da-Woon Jung and Woong-Hee Kim and Si-Hwan Park and Jinho Lee and Jinmi Kim and Dongdong Su and Hyung-Ho Ha and Y. -S. Chang and Darren Reece Williams},
  journal={ACS chemical biology},
  year={2013},
  volume={8 6},
  pages={1271-82}
}
Enolase is a component of the glycolysis pathway and a "moonlighting" protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule "ENOblock", which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small… CONTINUE READING