Introduction ON JUNE 24, 1971, Andrew V. Schally announced the determination of the primary structure of porcine GnRH at The Endocrine Society Meeting in San Francisco. This announcement was followed by publications by Matsuo et al. (1, 2) and Baba et al. (3) on the proposed amino acid sequence for porcine GnRH and its synthesis and by Burgus et al. (4) who characterized ovine GnRH and found the sequence to be identical with that of porcine GnRH. The physiological and therapeutic importance attributed to the discovery of the new substance was greatly increased by the prospect of the design of potent and long acting GnRH agonists and antagonists. Since that time more than 2000 analogs of GnRH have been synthesized. The impact of research of GnRH and its analogs on clinical medicine recently led Ziporyn (5) to note, “There's almost no subspecialty of medicine that will be left untouched by the [research] advances associated with LHRH or its analogs.” It is the intent of this article to provide a historical ...

Gonadotropin-releasing hormone analog design. Structure-function studies toward the development of agonists and antagonists: rationale and perspective.

I. Introduction II. Amino Acid Sequences of GnRH Receptors A. GnRH receptor cDNAs B. General structural features C. Covalent modifications D. Gene structure III. Structure-Activity Relations of GnRH Peptides A. Overview B. Comparative structures and activities of vertebrate GnRHs C. Roles of individual amino acids in GnRH activity at the mammalian receptor D. Conclusions from peptide structure-activity data IV. Structure and Conformation of GnRH and Its Analogs A. Early studies of GnRH conformation B. Integrated computational and experimental studies C. Exploration of the entire conformation space of GnRH analogs V. Functional Structure of the Receptor and Ligand-Receptor Complex A. Extracellular domains B. Helix domains C. Intracellular loop domains D. Computational modeling of three-dimensional receptor structure VI. Conclusions

/pdf/molecular-mechanisms-of-ligand-interaction-with-the-53djy3r057.pdf

Molecular Mechanisms of Ligand Interaction with the Gonadotropin-Releasing Hormone Receptor

GnRH analogues—agonists and antagonists

The sequencing and synthesis of mammalian lu teinizing hormone-releasing hormone (LHRH) 1-4 led to the expectation that this decapeptide would prove useful for therapy of infertility of hypothala mic origin. It was also forecast that substitution of some of the amino acids in the molecule might lead to competitive antagonists, useful as a new method of contraception. As it turned out, substitution led more quickly to increased agonist potency; many more years were to elapse before clinically evaluable antagonists appeared. LHRH is

Luteinizing Hormone - Releasing Hormone Analogs: Development and Mechanism of Action

PROBLEM: Gonadotropin-releasing hormone (GnRH) agonists are playing an increasing role in the medical management of a variety of diseases. Recent evidence also indicates GnRH immune system interactions.



METHOD: The present study investigated the sequential changes in lymphocyte subpopulations in secondary lymphoid tissues of prepubertal female mice in vivo following Lupron depot administration. A direct two-color immunofluorescence staining followed by flow cytometric analysis was employed.



RESULTS: Following agonist administration, white blood cell counts decreased significantly with decreases in both granulocyte and lymphocyte counts. Blood T-cell and B-cell subsets were also reduced although B cells decreased more markedly. In the spleen, B cells were again reduced more than T cells. There was no selective loss of either CD4 or CD8 subpopulations at any time point, in both spleen and blood. There were no differences in the percentage of lymph node subsets except that B cells decreased in the second week.



CONCLUSION: These data indicate that GnRH agonist alters specific lymphocyte subpopulations and, therefore, have the potential for affecting immune system function in vivo.

GnRH agonist induces suppression of lymphocyte subpopulations in secondary lymphoid tissues of prepubertal female mice.

Many methods for assaying the activity and potency of LHRH agonists and antagonists in the female have been developed. Considerably fewer assays have been done in males. Although several good comparisons of LHRH and its analogs have been conducted in male laboratory animals (Labrie et al., 1980), extensive potency studies on the reproductive effects of these peptides have been more conveniently assessed in females because the dosing schedules have been shorter and the endpoints more easily determined. Although the number and variations of the assays used to evaluate LHRH analogs have proliferated, they can be conveniently divided for ease of review into in vitro and in vivo assays.

Biological assays utilized to characterize LHRH and its analogs

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Biological assays utilized to characterize LHRH and its analogs