Identification of a conserved switch residue responsible for selective constitutive activation of the beta2-adrenergic receptor.

@article{Zuscik1998IdentificationOA,
  title={Identification of a conserved switch residue responsible for selective constitutive activation of the beta2-adrenergic receptor.},
  author={Micheal J Zuscik and Jill Porter and Robert J. Gaivin and Dianne Perez},
  journal={The Journal of biological chemistry},
  year={1998},
  volume={273 6},
  pages={3401-7}
}
A cysteine-to-phenylalanine mutation of residue 116 in the third transmembrane domain of the beta2-adrenergic receptor caused selective constitutive activation of Na+/H+ exchange through a pathway not involving cAMP. This selectivity was identified by comparing binding and signaling characteristics of wild-type (WT) versus C116F mutant receptors transiently transfected into COS-1 cells. Indicating constitutive activity, ligand binding to the C116F mutant showed a 78-fold higher than WT affinity… CONTINUE READING
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