Growth hormone receptor antagonists: discovery,development, and use in patients with acromegaly |
| |
| Authors: | Kopchick J J Parkinson C Stevens E C Trainer P J |
| |
| Institution: | Edison Biotechnology Institute, Department of Biomedical Sciences, College of Osteopathic Medicine, Ohio University, Athens, Ohio 45701, USA. |
| |
| 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. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
