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

  • J. J. Kopchick
  • , C. Parkinson
  • , E. C. Stevens
  • , P. J. Trainer

    Research output: Contribution to journalArticlepeer-review

    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.
    Original languageEnglish
    Pages (from-to)623-646
    Number of pages23
    JournalEndocrine Reviews
    Volume23
    Issue number5
    DOIs
    Publication statusPublished - Oct 2002

    UN SDGs

    This output contributes to the following UN Sustainable Development Goals (SDGs)

    1. SDG 3 - Good Health and Well-being
      SDG 3 Good Health and Well-being

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