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Related Experiment Videos

Glucocorticoid receptors.

G G Rousseau, J D Baxter

    Monographs on Endocrinology
    |January 1, 1979
    PubMed
    Summary
    This summary is machine-generated.

    Glucocorticoid receptors are intracellular proteins crucial for steroid hormone action. Their binding affinity and kinetics correlate with glucocorticoid effects, indicating they are rate-limiting factors in cellular responses.

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    Area of Science:

    • Endocrinology
    • Molecular Biology
    • Cell Biology

    Background:

    • Glucocorticoid receptors (GRs) are present in most mammalian tissues.
    • These receptors are primarily located in the cytoplasm in cells without steroid exposure.
    • Studying GRs relies on their high-affinity binding to radioactive steroids.

    Purpose of the Study:

    • To characterize the physicochemical properties of the glucocorticoid receptor.
    • To establish the correlation between receptor binding and physiological glucocorticoid action.
    • To investigate the role of GRs in cellular sensitivity to glucocorticoids.

    Main Methods:

    • Utilized radioactive steroids to study the binding kinetics and affinity of GRs.
    • Analyzed receptor properties including molecular weight, charge, and stability.

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  • Compared receptor characteristics across different cell lines and species.
  • Investigated the correlation between nuclear receptor binding and cellular response.

    • Main Results:

    • GRs are asymmetric, acidic proteins (~100,000 daltons), labile when unbound.
    • Binding follows Michaelian kinetics with approximately 10,000 sites per cell.
    • Receptor binding characteristics predict steroid analog activity and cellular responsiveness.
    • Nuclear binding of GRs strongly correlates with nuclear effects of glucocorticoids.
    • GR concentration appears unregulated by ligand or other hormones, but changes can affect sensitivity.

    Conclusions:

    • The identified protein is the physiologic glucocorticoid receptor, mediating steroid action.
    • GRs exist in inactive and active forms, with agonists promoting activation and nuclear translocation.
    • Receptor binding is a rate-limiting factor for glucocorticoid response magnitude and kinetics.
    • Understanding GRs is key to comprehending glucocorticoid regulation and sensitivity.