4,400 results found
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Common activation mechanism of class A GPCRs

    Qingtong Zhou et al.
    Contrary to previous findings, class A GPCRs share a common activation pathway that directly links ligand binding to G-protein activation, as revealed by novel quantitative analysis.
    1. Cell Biology
    2. Neuroscience

    The orphan receptor GPR88 blunts the signaling of opioid receptors and multiple striatal GPCRs

    Thibaut Laboute et al.
    GPR88 inhibits G-protein signaling of nearby GPCRs, and dampens b-arrestin recruitment by all GPCRs tested, likely by sequestration in intracellular compartments.
    1. Cell Biology
    2. Structural Biology and Molecular Biophysics

    Near-atomic structures of the BBSome reveal the basis for BBSome activation and binding to GPCR cargoes

    Shuang Yang et al.
    Membrane recruitment of BBSome is coupled to a conformational change, and interaction of the BBSome with GPCR cargoes depends on the GPCRs releasing their amphipathic helix 8 from the membrane.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Ligand modulation of sidechain dynamics in a wild-type human GPCR

    Lindsay D Clark et al.
    Generation of a highly deuterated 13C-methyl labeled wild-type GPCR sample is used to facilitate characterization of the molecular environments and fast ps-ns dynamics of sidechains when the receptor is bound to ligands of different efficacy.
    1. Structural Biology and Molecular Biophysics

    Molecular basis of signaling specificity between GIRK channels and GPCRs

    Kouki K Touhara, Roderick MacKinnon
    A single kinetic step in the G protein activation cycle determines whether a G protein-coupled receptor activates G protein-gated K+ channels or not.
    1. Cancer Biology
    2. Cell Biology

    Rac1-mediated membrane raft localization of PI3K/p110β is required for its activation by GPCRs or PTEN loss

    Onur Cizmecioglu et al.
    A unique two-step mechanism of plasma membrane recruitment and activation governs G-protein-coupled receptor mediated PI3K signaling.
    1. Neuroscience

    A striatal-enriched intronic GPCR modulates huntingtin levels and toxicity

    Yuwei Yao et al.
    A cell-surface receptor called Gpr52 is able to lower the levels of the disease-causing protein mutant huntingtin and suppress its toxicity when knocked-down, making this receptor a promising drug target in Huntington's disease.
    1. Developmental Biology
    2. Neuroscience

    The adhesion-GPCR BAI1 shapes dendritic arbors via Bcr-mediated RhoA activation causing late growth arrest

    Joseph G Duman et al.
    The adhesion-GPCR BAI1 shapes dendritic arbors in the hippocampus by associating with Bcr late in development and stimulating its RhoA-GEF activity, resulting in dendritic growth arrest.
    1. Cell Biology

    Phosphorylation of β-arrestin2 at Thr383 by MEK underlies β-arrestin-dependent activation of Erk1/2 by GPCRs

    Elisabeth Cassier et al.
    Phosphoproteomics identifies β-arrestin 2 phosphorylation at Thr383 by MEK as a key step of GPCR-induced Erk½ activation, thus providing new insight into the molecular mechanism underlying β-arrestin-dependent GPCR-operated signaling.
    1. Cancer Biology

    GPC1 specific CAR-T cells eradicate established solid tumor without adverse effects and synergize with anti-PD-1 Ab

    Daiki Kato et al.
    The safety and strong antitumor effects of GPC1-specific CAR-T cells against GPC1-expressing solid tumors were demonstrated by using both syngeneic and xenogeneic mouse models.

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