Reverse intrinsic activity of antagonists on G protein-coupled receptors.

@article{Schuetz1992ReverseIA,
  title={Reverse intrinsic activity of antagonists on G protein-coupled receptors.},
  author={Wilken Schuetz and Michael Freissmuth},
  journal={Trends in pharmacological sciences},
  year={1992},
  volume={13 10},
  pages={376-80}
}
Biological effects observed with an antagonist are usually interpreted as the result of its ability to block receptor activation produced by an endogenous agonist. In this Principles article, Wolfgang Schütz and Michael Freissmuth show how considerable evidence has now been accumulated for G protein-coupled receptors that antagonists not only bind to the receptor, but also induce a conformational change that favours uncoupling of the receptor from its G protein. The spontaneous activity of the… CONTINUE READING

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