Functional selective oxytocin-derived agonists discriminate between individual G protein family subtypes.

@article{Busnelli2012FunctionalSO,
  title={Functional selective oxytocin-derived agonists discriminate between individual G protein family subtypes.},
  author={Marta Busnelli and Aude Sauli{\`e}re and Maurice Manning and Michel Bouvier and C{\'e}line Gal{\'e}s and Bice Chini},
  journal={The Journal of biological chemistry},
  year={2012},
  volume={287 6},
  pages={3617-29}
}
We used a bioluminescence resonance energy transfer biosensor to screen for functional selective ligands of the human oxytocin (OT) receptor. We demonstrated that OT promoted the direct engagement and activation of G(q) and all the G(i/o) subtypes at the OT receptor. Other peptidic analogues, chosen because of specific substitutions in key OT structural/functional residues, all showed biased activation of G protein subtypes. No ligand, except OT, activated G(oA) or G(oB), and, with only one… CONTINUE READING

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