Identification of allosteric antagonists of receptor-guanine nucleotide-binding protein interactions.

@article{Huang1990IdentificationOA,
  title={Identification of allosteric antagonists of receptor-guanine nucleotide-binding protein interactions.},
  author={Ray R Huang and Robert N Dehaven and Ada Hoi-Fay Cheung and Ronald E. Diehl and Richard Alastair Dixon and Catherine D. Strader},
  journal={Molecular pharmacology},
  year={1990},
  volume={37 2},
  pages={304-10}
}
A series of compounds that inhibit the coupling of the alpha 2-adrenergic receptor and the beta 2-adrenergic receptor to the guanine nucleotide-binding proteins (G proteins) Gi and Gs, respectively, have been identified. This inhibition of G protein coupling was detected by the ability of the compounds to reduce the affinity of these receptors for agonists without affecting antagonist affinity. Analysis of the structure-activity relationships of these compounds revealed a requirement for… CONTINUE READING

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