2,689 results found
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein

    Javier García-Nafría et al.
    The adenosine A2a receptor couples to the heterotrimeric G protein Gs using both conserved contacts seen in other complexes and, in addition, novel contacts to the beta subunit of the G protein.
    1. Structural Biology and Molecular Biophysics
    2. Neuroscience

    C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor

    Anthony W Azevedo et al.
    Serine and threonine phosphorylation sites work in concert to provide rapid and reproducible desensitization of the G-protein coupled receptor rhodopsin.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Regulating G protein-coupled receptors by topological inversion

    Bray Denard et al.
    Multiple biochemical assays show that the topology of CCR5 and possibly other GPCRs may be inverted by ceramide or other sphingolipids through the process of regulated alternative translocation.
    1. Biochemistry and Chemical Biology
    2. Developmental Biology

    Cholesterol activates the G-protein coupled receptor Smoothened to promote Hedgehog signaling

    Giovanni Luchetti et al.
    Cholesterol regulates cell-cell communication by activating the Hedgehog pathway, a central signaling system in development, regeneration and cancer.
    1. Cancer Biology

    Activation of G protein-coupled estrogen receptor signaling inhibits melanoma and improves response to immune checkpoint blockade

    Christopher A Natale et al.
    Driving melanoma differentiation through G protein-coupled estrogen receptor signaling decreases proliferative capacity, decreases expression of the oncodriver and stem cell marker c-Myc, and increases the effectiveness of immunotherapy.
    1. Cell Biology

    G-protein-coupled receptors regulate autophagy by ZBTB16-mediated ubiquitination and proteasomal degradation of Atg14L

    Tao Zhang et al.
    Under normal nutritional conditions, G-protein coupled receptors can control autophagy by regulating the degradation of key autophagic regulator Atg14L through ZBTB16-mediated ubiquitination and proteasome degradation.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Computational design of thermostabilizing point mutations for G protein-coupled receptors

    Petr Popov et al.
    A comprehensive approach to prediction of stabilizing mutations in G-protein coupled receptors yields high hit rate and crystal structures of 5HT2C in both active and inactive states.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Cryo-EM structure of the rhodopsin-Gαi-βγ complex reveals binding of the rhodopsin C-terminal tail to the gβ subunit

    Ching-Ju Tsai et al.
    The structure of a light-sensitive G protein-coupled receptor in complex with a Gi-protein heterotrimer provides a structural foundation for the role of the receptor C-terminal tail in scaffolding and signaling.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Structural insight into the activation of a class B G-protein-coupled receptor by peptide hormones in live human cells

    Lisa Seidel et al.
    Agonist and antagonist peptides of the corticotropin-releasing factor receptor type 1 adopt different folds and stabilize distinct conformations of the receptor transmembrane domain, which involves tilting of helices VI and VII around conserved glycine hinges.
    1. Neuroscience

    Gi/o protein-coupled receptors in dopamine neurons inhibit the sodium leak channel NALCN

    Fabian Philippart, Zayd M Khaliq
    The sodium leak NALCN channel functions as a core effector of GABA-B and D2 receptors that is used along with GIRK channels to regulate action potential firing in dopamine neurons.

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