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Gonadotropin-releasing hormone receptors.

Gonadotropin-releasing hormone receptors. Research Abstract Details 

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  • Gonadotropin-releasing hormone receptors. Abstract Text:

    GnRH and its analogs are used extensively for the treatment of hormone-dependent diseases and assisted reproductive techniques. They also have potential as novel contraceptives in men and women. A thorough delineation of the molecular mechanisms involved in ligand binding, receptor activation, and intracellular signal transduction is kernel to understanding disease processes and the development of specific interventions. Twenty-three structural variants of GnRH have been identified in protochordates and vertebrates. In many vertebrates, three GnRHs and three cognate receptors have been identified with distinct distributions and functions. In man, the hypothalamic GnRH regulates gonadotropin secretion through the pituitary GnRH type I receptor via activation of G(q). In-depth studies have identified amino acid residues in both the ligand and receptor involved in binding, receptor activation, and translation into intracellular signal transduction. Although the predominant coupling of the type I GnRH receptor in the gonadotrope is through productive G(q) stimulation, signal transduction can occur via other G proteins and potentially by G protein-independent means. The eventual selection of intracellular signaling may be specifically directed by variations in ligand structure. A second form of GnRH, GnRH II, conserved in all higher vertebrates, including man, is present in extrahypothalamic brain and many reproductive tissues. Its cognate receptor has been cloned from various vertebrate species, including New and Old World primates. The human gene homolog of this receptor, however, has a frame-shift and stop codon, and it appears that GnRH II signaling occurs through the type I GnRH receptor. There has been considerable plasticity in the use of different GnRHs, receptors, and signaling pathways for diverse functions. Delineation of the structural elements in GnRH and the receptor, which facilitate differential signaling, will contribute to the development of novel interventive GnRH analogs.

    Gonadotropin-releasing hormone receptors. Publishing Authors By Initials

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    PUBMED ID PMID:

    MEDLINE DATE:

    Gonadotropin-releasing hormone receptors. Journal Published:

    PUBLICATION TYPE: Review

    Journal: Endocrine reviews

    VOLUME: 25

    Page Numbers: 235-75

    Journal Abbreviation: Endocr. Rev.

    ISSN: 0163-769X

    DAY: 6

    MONTH: Apr

    YEAR: 2004

    Gonadotropin-releasing hormone receptors. Information

    Number of References: 297

    LANGUAGE: eng

    NlmUniqueID: 8006258

    Gonadotropin-releasing hormone receptors. Keywords Mesh Terms:

    KEYWORDS: Signal Transduction

    MESH TERMS: physiology

    Chemical & Substance for Abstract: Gonadotropin-releasing hormone receptors. Information

    Substance Name: GTP-Binding Proteins

    Registry Number: EC 3.6.1.-

    Grant and Affiliation Information for Gonadotropin-releasing hormone receptors.

    AFFILIATION: Medical Research Council Human Reproductive Sciences Unit, Centre for Reproductive Biology, Chancellor's Building, 49 Little France Crescent, Edinburgh EH16 4SB, Scotland, United Kingdom. r.millar@hrsu.mrc.ac.uk

    Country: United States

    United States Research PublicationUnited States Research Publication

    AGENCY: United Kingdom Medical Re

    GRANT: U.1276.00.005.00002.

    ACRONYM:

    MEDLINETA: Endocr Rev

    REFSOURCE:

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    Number Hits: 0

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