G protein-coupled receptors

Definition

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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Latest Research and Reviews

  • Research |

    Crystal structures of hGPR40, a target for treatment of type 2 diabetes, bound to a partial and an allosteric agonist explain the binding cooperativity between these ligands and present new opportunities for structure-guided drug design.

    • Jun Lu
    • , Noel Byrne
    • , John Wang
    • , Gerard Bricogne
    • , Frank K Brown
    • , Harry R Chobanian
    • , Steven L Colletti
    • , Jerry Di Salvo
    • , Brande Thomas-Fowlkes
    • , Yan Guo
    • , Dawn L Hall
    • , Jennifer Hadix
    • , Nicholas B Hastings
    • , Jeffrey D Hermes
    • , Thu Ho
    • , Andrew D Howard
    • , Hubert Josien
    • , Maria Kornienko
    • , Kevin J Lumb
    • , Michael W Miller
    • , Sangita B Patel
    • , Barbara Pio
    • , Christopher W Plummer
    • , Bradley S Sherborne
    • , Payal Sheth
    • , Sarah Souza
    • , Srivanya Tummala
    • , Clemens Vonrhein
    • , Maria Webb
    • , Samantha J Allen
    • , Jennifer M Johnston
    • , Adam B Weinglass
    • , Sujata Sharma
    •  & Stephen M Soisson
  • Research |

    The structure of the GLP-1 receptor complexed with its ligand offers insight into the mechanism of class B G-protein-coupled receptor activation.

    • Yan Zhang
    • , Bingfa Sun
    • , Dan Feng
    • , Hongli Hu
    • , Matthew Chu
    • , Qianhui Qu
    • , Jeffrey T. Tarrasch
    • , Shane Li
    • , Tong Sun Kobilka
    • , Brian K. Kobilka
    •  & Georgios Skiniotis
    Nature 546, 248–253
  • Research | | open

    Nutrients taste perception is mediated by T1r receptors that discriminate specific tastes among their wide diversity. Here the authors present crystal structures of the ligand-binding domains of the fish T1r2-T1r3 receptor, providing a structural framework for its ligand recognition.

    • Nipawan Nuemket
    • , Norihisa Yasui
    • , Yuko Kusakabe
    • , Yukiyo Nomura
    • , Nanako Atsumi
    • , Shuji Akiyama
    • , Eriko Nango
    • , Yukinari Kato
    • , Mika K. Kaneko
    • , Junichi Takagi
    • , Maiko Hosotani
    •  & Atsuko Yamashita
  • Research |

    Membrane curvature induces sorting of GPCRs within live-cell-membrane protrusions, and the curvature-dependent sorting is affected by agonist binding. Thermodynamic modeling suggests that this is due to an energetic drive to match receptor shape and elasticity to membrane curvature.

    • Kadla R Rosholm
    • , Natascha Leijnse
    • , Anna Mantsiou
    • , Vadym Tkach
    • , Søren L Pedersen
    • , Volker F Wirth
    • , Lene B Oddershede
    • , Knud J Jensen
    • , Karen L Martinez
    • , Nikos S Hatzakis
    • , Poul Martin Bendix
    • , Andrew Callan-Jones
    •  & Dimitrios Stamou

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