G protein-coupled receptors articles from across Nature Portfolio

G protein-coupled receptors (GPCRs) are integral membrane proteins with seven membrane-spanning helices. Upon binding to a ligand – which can range from small molecules like cyclic AMP to peptides and large proteins – GPCRs undergo a conformational change that activates heterotrimeric G proteins (guanine nucleotide-binding proteins), which are important for transmitting the extracellular, ligand signal to the cell interior.

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News and Comment

  • News & Views |

    GPCRs are selective for specific G-protein subtypes, thereby ensuring signaling fidelity. A new report finds that that empty-like G-protein mutants are promiscuously recognized by GPCRs, suggesting that receptors select cognate over non-cognate G proteins at steps preceding nucleotide release.

    • Mikel Garcia-Marcos
  • News & Views |

    Inflamed tissue has a special milieu, with hypoxia, high levels of metabolites from anaerobic glycolysis, and acidosis. Stimulation of a proton-activated receptor, TDAG8 (GPR65), in T cells has an important role in inflammatory bowel disease by balancing pro- and anti-inflammatory signals.

    • Carsten A. Wagner
    •  & Pedro H. Imenez Silva
    Nature Immunology 23, 991-993
  • News & Views |

    Cryo-EM structures of Mas-related G-protein-coupled receptors (MRGPRs) that are involved in the allergic reaction and itch response reveal structural insights into their activation mechanism, and offer the potential to discover new therapeutic agents for pain and hypersensitivity reactions.

    • Jagannath Maharana
    • , Parishmita Sarma
    •  & Arun K. Shukla
  • News & Views |

    Targeting cholecystokinin receptors (CCKRs) signaling has become an attractive therapeutic strategy for many diseases. The description of cryo-EM structures of CCKRs in the active or inactive states reveal the molecular mechanism of ligand recognition and G-protein-coupling promiscuity.

    • Lin Cheng
    •  & Zhenhua Shao
    Nature Chemical Biology 17, 1213-1214