Conversion of a gonadotropin-releasing hormone antagonist to an agonist

  title={Conversion of a gonadotropin-releasing hormone antagonist to an agonist},
  author={P. M. Conn and D. C. Rogers and J. Stewart and J. Niedel and T. Sheffield},
  • P. M. Conn, D. C. Rogers, +2 authors T. Sheffield
  • Published 1982
  • Chemistry, Medicine
  • Nature
  • Gonadotropin-releasing hormone (pyroGlu1-His2-Trp3-Ser4-Tyr5-Gly6-Leu7-Arg8-Pro9-Gly10 amide, GnRH) stimulates pituitary luteinizing hormone (LH) release. An antagonist, D-pyroGlu1-D-Phe2-D-Trp3-D-Lys6-GnRH (GnRH-Ant), binds to the pituitary GnRH receptor and inhibits GnRH-stimulated (10−9 M) gonadotropin release from pituitary cultures (IC50 = 2 × 10×7 M). GnRH-Ant has no measurable agonist activity at concentrations up to 10−6 M. The presence of the D-Lys6 both affords protection against… CONTINUE READING
    169 Citations

    Topics from this paper.

    Gonadotropin releasing-hormone receptors: photoaffinity labeling with an antagonist.
    • E. Hazum, D. Keinan
    • Chemistry, Medicine
    • Biochemical and biophysical research communications
    • 1983
    • 13
    Gonadotropin releasing hormone activation is mediated by dimerization of occupied receptors.
    • E. Hazum, D. Keinan
    • Biology, Medicine
    • Biochemical and biophysical research communications
    • 1985
    • 19
    Gonadotrophin-releasing hormone: physiological significance and relevance to cancer.
    • 6
    Structural and functional evolution of gonadotropin-releasing hormone.
    • 56
    Enhanced biological activity of dimeric gonadotropin releasing hormone.
    • 4


    Gonadotropin-releasing hormone action in the pituitary: a three step mechanism.
    • 181
    • PDF
    Receptor-mediated internalization of fluorescent gonadotropin-releasing hormone by pituitary gonadotropes.
    • 146
    • PDF
    Direct demonstration that receptor crosslinking or aggregation is important in insulin action.
    • 328
    • PDF