Inverse, protean, and ligand‐selective agonism: matters of receptor conformation

@article{Kenakin2001InversePA,
  title={Inverse, protean, and ligand‐selective agonism: matters of receptor conformation},
  author={Terry Kenakin},
  journal={The FASEB Journal},
  year={2001},
  volume={15},
  pages={589 - 611}
}
  • T. Kenakin
  • Published 2001
  • Biology, Medicine
  • The FASEB Journal
Concepts regarding the mechanisms by which drugs activate receptors to produce physiological response have progressed beyond considering the re¬ceptor as a simple on‐off switch. Current evidence suggests that the idea that agonists produce only vary¬ing degrees of receptor activation is obsolete and must be reconciled with data to show that agonist efficacy has texture as well as magnitude. Thus, agonists can block system constitutive response (inverse agonists), behave as positive and inverse… Expand
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  • Biology, Medicine
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