Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature

J Clin Invest. 2006 Mar;116(3):760-8. doi: 10.1172/JCI25303.

Abstract

The growth hormone (GH) secretagogue receptor (GHSR) was cloned as the target of a family of synthetic molecules endowed with GH release properties. As shown recently through in vitro means, this receptor displays a constitutive activity whose clinical relevance is unknown. Although pharmacological studies have demonstrated that its endogenous ligand--ghrelin--stimulates, through the GHSR, GH secretion and appetite, the physiological importance of the GHSR-dependent pathways remains an open question that gives rise to much controversy. We report the identification of a GHSR missense mutation that segregates with short stature within 2 unrelated families. This mutation, which results in decreased cell-surface expression of the receptor, selectively impairs the constitutive activity of the GHSR, while preserving its ability to respond to ghrelin. This first description, to our knowledge, of a functionally significant GHSR mutation, which unveils the critical importance of the GHSR-associated constitutive activity, discloses an unusual pathogenic mechanism of growth failure in humans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Amino Acid Sequence
  • Amino Acid Substitution / genetics
  • Animals
  • Body Height / genetics*
  • Cell Line
  • Child
  • Female
  • Ghrelin
  • Growth Disorders / genetics*
  • Humans
  • Male
  • Middle Aged
  • Molecular Sequence Data
  • Mutation, Missense*
  • Pedigree
  • Peptide Hormones / metabolism
  • Peptide Hormones / physiology
  • Receptors, G-Protein-Coupled / deficiency*
  • Receptors, G-Protein-Coupled / genetics*
  • Receptors, G-Protein-Coupled / physiology
  • Receptors, Ghrelin

Substances

  • Ghrelin
  • Peptide Hormones
  • Receptors, G-Protein-Coupled
  • Receptors, Ghrelin