Predicted Michaelis-Menten complexes of cocaine-butyrylcholinesterase. Engineering effective butyrylcholinesterase mutants for cocaine detoxication.

@article{Sun2001PredictedMC,
  title={Predicted Michaelis-Menten complexes of cocaine-butyrylcholinesterase. Engineering effective butyrylcholinesterase mutants for cocaine detoxication.},
  author={Hong Xue Sun and J El Yazal and Oksana Lockridge and Lawrence M. Schopfer and Stephen Brimijoin and Yuan Ping Pang},
  journal={The Journal of biological chemistry},
  year={2001},
  volume={276 12},
  pages={9330-6}
}
Butyrylcholinesterase (BChE) is important in cocaine metabolism, but it hydrolyzes (-)-cocaine only one-two thousandth as fast as the unnatural (+)-stereoisomer. A starting point in engineering BChE mutants that rapidly clear cocaine from the bloodstream, for overdose treatment, is to elucidate structural factors underlying the stereochemical difference in catalysis. Here, we report two three-dimensional Michaelis-Menten complexes of BChE liganded with natural and unnatural cocaine molecules… CONTINUE READING

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