An overview of the diverse roles of G-protein coupled receptors (GPCRs) in the pathophysiology of various human diseases

Biotechnol Adv. 2013 Dec;31(8):1676-94. doi: 10.1016/j.biotechadv.2013.08.017. Epub 2013 Aug 30.


G-protein coupled receptors (GPCRs) modulate diverse cellular responses to the majority of neurotransmitters and hormones within the human body. They exhibit much structural and functional diversity, and are responsive to a plethora of endogenous (biogenic amines, cations, lipids, peptides, and glycoproteins) and exogenous (therapeutic drugs, photons, tastants, and odorants) ligands and stimuli. Due to the key roles of GPCRs in tissue/cell physiology and homeostasis, signaling pathways associated with GPCRs are implicated in the pathophysiology of various diseases, ranging from metabolic, immunological, and neurodegenerative disorders, to cancer and infectious diseases. Approximately 40% of clinically approved drugs mediate their effects by modulating GPCR signaling pathways, which makes them attractive targets for drug screening and discovery. The pace of discovery of new GPCR-based drugs has recently accelerated due to rapid advancements in high-resolution structure determination, high-throughput screening technology and in silico computational modeling of GPCR binding interaction with potential drug molecules. This review aims to provide an overview of the diverse roles of GPCRs in the pathophysiology of various diseases that are the major focus of biopharmaceutical research as potential drug targets.

Keywords: Disease; G-protein; Human; Molecular; Pathology; Receptor.

Publication types

  • Review

MeSH terms

  • Cardiovascular Diseases / physiopathology*
  • Communicable Diseases / physiopathology
  • Humans
  • Immune System Diseases / physiopathology*
  • Metabolic Diseases / physiopathology*
  • Neoplasms / physiopathology*
  • Neurodegenerative Diseases / physiopathology
  • Receptors, G-Protein-Coupled*


  • Receptors, G-Protein-Coupled