Growth Hormone Antagonists. A Pharmacological Tool in Present and Future Therapies
Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Growth Hormone Antagonists. A Pharmacological Tool in Present and Future Therapies. / Kopchick, John J.; Qiu, Lingua; Gosney, Elahu; Keller, Chad; Palmer, Amanda; Sankaran, Sudha.
The Somatotrophic Axis in Brain Function. Elsevier Science Inc., 2005. p. 313-326.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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TY - CHAP
T1 - Growth Hormone Antagonists. A Pharmacological Tool in Present and Future Therapies
AU - Kopchick, John J.
AU - Qiu, Lingua
AU - Gosney, Elahu
AU - Keller, Chad
AU - Palmer, Amanda
AU - Sankaran, Sudha
PY - 2005/12/1
Y1 - 2005/12/1
N2 - This chapter discusses the experimental methodologies that resulted in the discovery of growth hormone antagonists (GHAs). It also examines the in vitro and in vivo data that led to the approval of clinical use of GHA (pegvisomant). The structure-function analysis of growth hormone (GH) resulted in the discovery of a growth hormone antagonist. The antagonistic activity of the GH analogs provides the basis for development of the GHA as a new type of drug. The GHA competes with native GH and inhibits its proper or functional binding to and activation of GH receptors. Subsequent development of a Pegvisomant resulted in a novel drug for the treatment of acromegalic individuals. The ability of Pegvisomant to normalize elevated circulating IGF-I levels in patients with acromegaly serves as a new therapeutic approach toward this disorder. Furthermore, the chapter illustrates the potential role of GHAs in the treatment of certain types of cancer, as an insulin sensitizer, and in treatment of diabetes end organ damage.
AB - This chapter discusses the experimental methodologies that resulted in the discovery of growth hormone antagonists (GHAs). It also examines the in vitro and in vivo data that led to the approval of clinical use of GHA (pegvisomant). The structure-function analysis of growth hormone (GH) resulted in the discovery of a growth hormone antagonist. The antagonistic activity of the GH analogs provides the basis for development of the GHA as a new type of drug. The GHA competes with native GH and inhibits its proper or functional binding to and activation of GH receptors. Subsequent development of a Pegvisomant resulted in a novel drug for the treatment of acromegalic individuals. The ability of Pegvisomant to normalize elevated circulating IGF-I levels in patients with acromegaly serves as a new therapeutic approach toward this disorder. Furthermore, the chapter illustrates the potential role of GHAs in the treatment of certain types of cancer, as an insulin sensitizer, and in treatment of diabetes end organ damage.
UR - http://www.scopus.com/inward/record.url?scp=84882490407&partnerID=8YFLogxK
U2 - 10.1016/B978-012088484-1/50027-6
DO - 10.1016/B978-012088484-1/50027-6
M3 - Book chapter
SN - 9780120884841
SP - 313
EP - 326
BT - The Somatotrophic Axis in Brain Function
PB - Elsevier Science Inc.
ER -
ID: 202372161