A critical pocket close to the glutamate binding site of mGlu receptors opens new possibilities for agonist design.

@article{Acher2011ACP,
  title={A critical pocket close to the glutamate binding site of mGlu receptors opens new possibilities for agonist design.},
  author={Francine C Acher and Chelliah Selvam and Jean-Philippe Pin and Cyril Goudet and Hugues-Olivier Bertrand},
  journal={Neuropharmacology},
  year={2011},
  volume={60 1},
  pages={102-7}
}
A recent publication from Ogawa et al. suggested a possible allosteric chloride binding site in the extracellular domain of metabotropic glutamate receptors (mGluRs) by comparison with a similar site found in atrial natriuretic peptide receptor. We simultaneously reported about (S)-PCEP an agonist of subtype 4 mGluR that would bind to a similar pocket, adjacent to the glutamate binding site. Here we disclose LSP1-2093, a new derivative of (S)-PCEP that holds a nitrophenyl substituent. Docking… CONTINUE READING