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    Growth hormone receptor antagonists: discovery, development, and use in patients with acromegaly.

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    Authors
    Kopchick, J J
    Parkinson, Craig
    Stevens, E C
    Trainer, Peter J
    Affiliation
    Edison Biotechnology Institute, Department of Biomedical Sciences, College of Osteopathic Medicine, Ohio University, Athens, Ohio 45701, USA.
    Issue Date
    2002-10
    
    Metadata
    Show full item record
    Abstract
    An understanding of the events that occur during GH receptor (GHR) signaling has facilitated the development of a GHR antagonist (pegvisomant) for use in humans. This molecule has been designed to compete with native GH for the GHR and to prevent its proper or functional dimerization-a process that is critical for GH signal transduction and IGF-I synthesis and secretion. Clinical trials in patients with acromegaly show GHR blockade to be an exciting new mode of therapy for this condition, and pegvisomant may have a therapeutic role in diseases, such as diabetes and malignancy, in which abnormalities of the GH/IGF-I axis have been observed. This review charts the discovery and development of GHR antagonists and details the experience gained in patients with acromegaly.
    Citation
    Growth hormone receptor antagonists: discovery, development, and use in patients with acromegaly. 2002, 23 (5):623-46 Endocr. Rev.
    Journal
    Endocrine Reviews
    URI
    http://hdl.handle.net/10541/80243
    PubMed ID
    12372843
    Type
    Article
    Language
    en
    ISSN
    0163-769X
    Collections
    All Christie Publications

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