High constitutive activity is an intrinsic feature of ghrelin receptor protein: a study with a functional monomeric GHS-R1a receptor reconstituted in lipid discs.

@article{Damian2012HighCA,
  title={High constitutive activity is an intrinsic feature of ghrelin receptor protein: a study with a functional monomeric GHS-R1a receptor reconstituted in lipid discs.},
  author={Marjorie Damian and Jacky Marie and Jean-Philippe Leyris and Jean-Alain Fehrentz and Pascal Verdi{\'e} and Jean Paul Ruiz Mart{\'i}nez and Jean-Louis Ban{\`e}res and Sophie Mary},
  journal={The Journal of biological chemistry},
  year={2012},
  volume={287 6},
  pages={
          3630-41
        }
}
Despite its central role in signaling and the potential therapeutic applications of inverse agonists, the molecular mechanisms underlying G protein-coupled receptor (GPCR) constitutive activity remain largely to be explored. In this context, ghrelin receptor GHS-R1a is a peculiar receptor in the sense that it displays a strikingly high, physiologically relevant, constitutive activity. To identify the molecular mechanisms responsible for this high constitutive activity, we have reconstituted a… CONTINUE READING

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References

Publications referenced by this paper.
SHOWING 1-10 OF 71 REFERENCES

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

X. J. Yao, G. Vélez Ruiz, +5 authors B. Kobilka
  • Proc. Natl. Acad. Sci. U.S.A
  • 2009
VIEW 18 EXCERPTS
HIGHLY INFLUENTIAL