Rescue of expression and signaling of human luteinizing hormone G protein-coupled receptor mutants with an allosterically binding small-molecule agonist.

@article{Newton2011RescueOE,
  title={Rescue of expression and signaling of human luteinizing hormone G protein-coupled receptor mutants with an allosterically binding small-molecule agonist.},
  author={Claire L Newton and Adele M Whay and Craig Alexander McArdle and Meilin Zhang and Chris J van Koppen and Ruud van de Lagemaat and Deborah L Segaloff and Robert Peter Millar},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2011},
  volume={108 17},
  pages={7172-6}
}
Naturally occurring mutations of G protein-coupled receptors (GPCRs) causing misfolding and failure to traffic to the cell surface can result in disease states. Some small-molecule orthosteric ligands can rescue such misfolded receptors, presumably by facilitating their correct folding and shuttling to the plasma membrane. Here we show that a cell-permeant, allosterically binding small-molecule agonist (Org 42599) rescues the folding and cell surface expression, and therefore target cell… CONTINUE READING

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