Identification of Determinants Required for Agonistic and Inverse Agonistic Ligand Properties at the ADP Receptor P2Y12

  title={Identification of Determinants Required for Agonistic and Inverse Agonistic Ligand Properties at the ADP Receptor P2Y12},
  author={Philipp Schmidt and Lars Ritscher and Elizabeth N. Dong and Thomas Hermsdorf and Maxi C{\"o}ster and Doreen Wittkopf and Jens Meiler and Torsten Sch{\"o}neberg},
  journal={Molecular Pharmacology},
  pages={256 - 266}
The ADP receptor P2Y12 belongs to the superfamily of G protein–coupled receptors (GPCRs), and its activation triggers platelet aggregation. Therefore, potent antagonists, such as clopidogrel, are of high clinical relevance in prophylaxis and treatment of thromboembolic events. P2Y12 displays an elevated basal activity in vitro, and as such, inverse agonists may be therapeutically beneficial compared with antagonists. Only a few inverse agonists of P2Y12 have been described. To expand this… 

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    Proceedings of the National Academy of Sciences of the United States of America
  • 2006
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