Ghrelin Receptor Antagonists Small Molecules and Peptides

Ghrelin is the endogenous ligand for the ghrelin receptor, also known as the growth hormone secretagog receptor (GHS-R1a). Alternative splicing of the preproghrelin yields two active peptides: ghrelin and des-Gln¹⁴-ghrelin, which differ by the deletion of one amino acid residue. The predominant form, ghrelin, is highly expressed in endocrine cells of the stomach, with low levels also found in the hypothalamus.

The G-protein-coupled ghrelin receptor is expressed in the pituitary, hypothalamus, ...