Biological, Physiological, Pathophysiological, and Pharmacological Aspects of Ghrelin
Aart J. van der Lely,
Matthias Tschöp,
Mark L. Heiman and
Ezio Ghigo
Division of Endocrinology and Metabolism (A.J.v.d.L.), Department of Internal Medicine, Erasmus Medical Center, 3015 GD Rotterdam, The Netherlands; Department of Psychiatry (M.T.), University of Cincinnati, Cincinnati, Ohio 45237; Endocrine Research Department (M.L.H.), Eli Lilly and Co., Indianapolis, Indiana 46285; and Division of Endocrinology (E.G.), Department of Internal Medicine, University of Turin, Turin, Italy 10095
Correspondence: Address all correspondence and requests for reprints to: Aart Jan van der Lely, M.D., Department of Internal Medicine, Erasmus Medical Center, 40 Dr. Molewaterplein, 3015 GD Rotterdam, The Netherlands. E-mail: a.vanderlelij{at}erasmusmc.nl
Ghrelin is a peptide predominantly produced by the stomach.Ghrelin displays strong GH-releasing activity. This activityis mediated by the activation of the so-called GH secretagoguereceptor type 1a. This receptor had been shown to be specificfor a family of synthetic, peptidyl and nonpeptidyl GH secretagogues.Apart from a potent GH-releasing action, ghrelin has other activitiesincluding stimulation of lactotroph and corticotroph function,influence on the pituitary gonadal axis, stimulation of appetite,control of energy balance, influence on sleep and behavior,control of gastric motility and acid secretion, and influenceon pancreatic exocrine and endocrine function as well as onglucose metabolism. Cardiovascular actions and modulation ofproliferation of neoplastic cells, as well as of the immunesystem, are other actions of ghrelin. Therefore, we considerghrelin a gastrointestinal peptide contributing to the regulationof diverse functions of the gut-brain axis. So, there is indeeda possibility that ghrelin analogs, acting as either agonistsor antagonists, might have clinical impact.
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