Drug efficacy at G protein-coupled receptors.

@article{Kenakin2002DrugEA,
  title={Drug efficacy at G protein-coupled receptors.},
  author={Terry Kenakin},
  journal={Annual review of pharmacology and toxicology},
  year={2002},
  volume={42},
  pages={349-79}
}
  • Terry Kenakin
  • Published 2002 in Annual review of pharmacology and toxicology
Efficacy has been defined in receptor pharmacology as a proportionality factor denoting the amount of physiological response a given ligand imparts to a biological system for a given amount of receptor occupancy. While first defined in terms of response, the concept can be expanded to a wide variety of G protein-coupled receptor (GPCR) behaviors, which includes pleiotropic interaction with multiple G proteins, internalization, oligomerization, desensitization, and interaction with membrane… CONTINUE READING

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