GPCRs and Endocrinology

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G-protein-coupled receptors (GPCRs) form the largest family of receptors in humans, with over 800 members. These receptors mediate the effects of many hormones and convey numerous endocrine functions including growth, appetite regulation, bone development, glucose homeostasis and reproduction. Consequently, mutations in these receptors cause a spectrum of disorders and studies of these diseases has provided new insights into GPCR functions. This has led to an enhanced appreciation of the complexity of GPCR signaling achieved, in part, by the ability of receptors to couple to multiple G-protein pathways, utilization of sophisticated spatiotemporal signaling from plasma membrane and intracellular compartments, oligomerization of receptors and activation of G-protein-independent pathways. Pharmacological strategies for targeting GPCRs have become increasingly nuanced with the development of chimeric ligands targeting multiple receptors and the emergence of compounds that enable biased signaling. Future therapeutic approaches are likely to further enhance tissue and functional specificity. This article focusses on GPCRs involved in energy metabolism and growth (melanocortin, ghrelin, somatostatin, GLP-1 and GIP receptors); calcium homeostasis and skeletal development (calcium-sensing and parathyroid hormone receptors); thyroid function (TSH receptor); and reproduction (GnRHR, LHR, FSHR, KISS1R). Mutations in these GPCRs contribute to diverse human disorders including severe obesity, hyper/hypocalcaemia, skeletal dysplasia, hyper/hypothyroidism, precocious puberty, and delayed sexual development, and many are targets for currently approved drugs. For each receptor an understanding of the biological function, signal transduction mechanisms and pathophysiological consequences of human mutations will be explained, and current and future therapeutic strategies for targeting each receptor described.
Original languageEnglish
Title of host publicationReference Module in Biomedical Sciences
Publication statusPublished - 30 Jan 2021


  • Appetite regulation
  • Biased signaling
  • Calcium and phosphate homeostasis
  • Calcium-sensing receptor
  • Ghrelin receptor
  • Glucagon-like peptide-1 receptor
  • Glucose homeostasis
  • Gonadotropin receptors
  • Gonadotropin-releasing hormone receptor
  • Kisspeptin receptor
  • Melanocortin receptors
  • Parathyroid hormone receptor
  • Somatostatin receptor
  • Thyroid-stimulating hormone receptor


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