Growth hormone and glucose metabolism: the model of the GH-receptor antagonists.
Pegvisomant is a GH analogue that includes a single amino acid substitution at position 120 that generates the GHR antagonist. Additional changes include amino acid substitutions within binding site 1 and a further modification by the addition of polyethylene glycol moieties that increase the half-life and reduce the immunogenicity of the molecule. In acromegalics, pegvisomant is the most effective treatment for normalizing the IGF-I, and pegvisomant significantly improves insulin sensitivity in patients suffering from acromegaly. However, there are simply no data available that might support a role for pegvisomant treatment in disorders in which glucose metabolism is disturbed and in which reducing GH action would be theoretically beneficial.
Van der Lely
A J
AJ
Division of Endocrinology and Metabolism, Department of Internal Medicine, Erasmus Medical Center, 40 Dr Molewaterplein, 3015 GD Rotterdam, the Netherlands. a.vanderlelij@erasmusmc.nl
D000818:Animals; D003920:Diabetes Mellitus / Q000503:physiopathology; D005947:Glucose / Q000378:metabolism*; D013006:Growth Hormone / Q000502:physiology*; D019382:Human Growth Hormone / Q000378:metabolism / Q000502:physiology*; D006801:Humans; D011986:Receptors, Somatotropin / Q000037:antagonists & inhibitors / Q000502:physiology*
D011986:Receptors, Somatotropin; D019382:Human Growth Hormone; D013006:Growth Hormone; D005947:Glucose