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This gene encodes a protein that is a transmembrane receptor for growth hormone. [10] [11] Binding of growth hormone to the receptor leads to reorientation of a pre-assembled receptor dimer dimerization (the receptor may however also exist as monomers on the cell surface [12]) and the activation of an intra- and intercellular signal transduction pathway leading to growth. [13]
The GnRH antagonist abarelix was withdrawn from the United States market in 2005 and is now only marketed in Germany for use in patients with symptomatic prostate cancer. Degarelix is a GnRH antagonist that is approved for use in patients with advanced hormone-sensitive prostate cancer throughout Europe and also in the United States. [2]
Pegvisomant, sold under the brand name Somavert, is a growth hormone receptor antagonist used in the treatment of acromegaly. [1] [2] [3] It is primarily used if the pituitary gland tumor causing the acromegaly cannot be controlled with surgery or radiation, and the use of somatostatin analogues is unsuccessful, but is also effective as a monotherapy. [4]
The latest development in the medical treatment of acromegaly is the use of growth hormone receptor antagonists. The only available member of this family is pegvisomant (Somavert). By blocking the action of the endogenous growth hormone molecules, this compound is able to control the disease activity of acromegaly in virtually everyone with ...
Hormone receptor antagonists bind to the normal receptor for a given hormone and prevent its activation. The target receptor may be on the cell surface, as in the case of peptide and glycoprotein hormones, or it may be intracellular, as in the case of steroid hormone receptors. [citation needed]
[citation needed] Although cabergoline is commonly described principally as a D 2 receptor agonist, it also possesses significant affinity for the dopamine D 3, and D 4, serotonin 5-HT 1A, 5-HT 2A, 5-HT 2B, and 5-HT 2C, and α 2-adrenergic receptors, as well as moderate/low affinity for the dopamine D 1, serotonin 5-HT 7, and α 1-adrenergic ...
Growth hormone secretagogue receptor(GHS-R), also known as ghrelin receptor, is a G protein-coupled receptor that binds growth hormone secretagogues (GHSs), such as ghrelin, the "hunger hormone". [ 5 ] [ 6 ] The role of GHS-R is thought to be in regulating energy homeostasis and body weight. [ 7 ]
The growth-hormone-releasing hormone receptor (GHRHR) is a G-protein-coupled receptor that binds growth hormone-releasing hormone. The GHRHR activates a Gs protein that causes a cascade of cAMP via adenylate cyclase . [ 5 ]
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