Ghrelin receptor signaling in health and disease: a biased view

Joshua D. Gross, Yang Zhou, Lawrence S. Barak, Marc G. Caron

Research output: Contribution to journalReview articlepeer-review

5 Scopus citations


As allosteric complexes, G-protein-coupled receptors (GPCRs) respond to extracellular stimuli and pleiotropically couple to intracellular transducers to elicit signaling pathway-dependent effects in a process known as biased signaling or functional selectivity. One such GPCR, the ghrelin receptor (GHSR1a), has a crucial role in restoring and maintaining metabolic homeostasis during disrupted energy balance. Thus, pharmacological modulation of GHSR1a bias could offer a promising strategy to treat several metabolism-based disorders. Here, we summarize current evidence supporting GHSR1a functional selectivity in vivo and highlight recent structural data. We propose that precise determinations of GHSR1a molecular pharmacology and pathway-specific physiological effects will enable discovery of GHSR1a drugs with tailored signaling profiles, thereby providing safer and more effective treatments for metabolic diseases.

Original languageEnglish (US)
Pages (from-to)106-118
Number of pages13
JournalTrends in Endocrinology and Metabolism
Issue number2
StatePublished - Feb 2023

All Science Journal Classification (ASJC) codes

  • Endocrinology, Diabetes and Metabolism
  • Endocrinology

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