Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective.

@article{Milligan2003ConstitutiveAA,
  title={Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective.},
  author={Graeme Milligan},
  journal={Molecular pharmacology},
  year={2003},
  volume={64 6},
  pages={
          1271-6
        }
}
  • Graeme Milligan
  • Published in Molecular pharmacology 2003
  • Medicine, Chemistry
  • Over the last decade, the ability to detect agonist-independent signal transduction by G protein-coupled receptors has in turn resulted in the detection and study of ligands able to block this activity. Such ligands are generically described as inverse agonists. Considerable attention has recently been devoted to the presence and roles of endogenous antagonist/inverse agonists and the concept that inverse agonists may have specific therapeutic benefits compared with neutral antagonists. 

    Topics from this paper.

    Citations

    Publications citing this paper.
    SHOWING 1-10 OF 140 CITATIONS, ESTIMATED 44% COVERAGE

    Signaling pathways in melanosome biogenesis and pathology.

    VIEW 21 EXCERPTS
    CITES RESULTS
    HIGHLY INFLUENCED

    Single-molecule view of basal activity and activation mechanisms of the G protein-coupled receptor β2AR.

    VIEW 6 EXCERPTS
    CITES BACKGROUND
    HIGHLY INFLUENCED

    Identification of a potent inverse agonist at a constitutively active mutant of human P2Y12 receptor.

    VIEW 11 EXCERPTS
    CITES BACKGROUND
    HIGHLY INFLUENCED

    The fall and rise of pharmacology--(re-)defining the discipline?

    VIEW 16 EXCERPTS
    CITES BACKGROUND
    HIGHLY INFLUENCED

    In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor?

    VIEW 4 EXCERPTS
    CITES BACKGROUND
    HIGHLY INFLUENCED

    Role of the G-Protein-Coupled Receptor Signaling Pathway in Insecticide Resistance

    VIEW 2 EXCERPTS
    CITES BACKGROUND

    FILTER CITATIONS BY YEAR

    2004
    2019

    CITATION STATISTICS

    • 8 Highly Influenced Citations

    • Averaged 7 Citations per year from 2017 through 2019

    References

    Publications referenced by this paper.
    SHOWING 1-10 OF 76 REFERENCES

    Genomewide view of gene silencing by small interfering RNAs.

    VIEW 2 EXCERPTS