An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials.

Ghrelin is a multifunctional gastrointestinal acylated peptide, primarily synthesized in the stomach and regulates the secretion of growth hormone and energy homeostasis. It plays a central role in modulating the diverse biological, physiological and pathological functions in vertebrates. The synthesis of ghrelin receptor ligands after the finding of growth hormone secretagogue developed from Met-enkephalin led to reveal the endogenous ligand ghrelin and the receptors. Subsequently, many peptides, small molecules and peptidomimetics focusing on the ghrelin receptor, GHS-R1a, were derived. In this review, the key features of ghrelin's structure, forms, its bio-physiological functions, pathological roles and therapeutic potential have been highlighted. A few peptidomimetics and pseudo peptide synthetic perspectives have also been discussed to make ghrelin receptor ligands, clinical trials and their success.