419 results found
    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. Human Biology and Medicine
    2. 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. 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. 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. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Viral GPCR US28 can signal in response to chemokine agonists of nearly unlimited structural degeneracy

    Timothy F Miles et al.
    Numerous chemokine variants bearing no sequence resemblance elicit similar signaling behavior from the viral GPCR US28, suggesting a mechanism for receptor activation that accommodates extensive ligand degeneracy.
    1. Biochemistry and Chemical Biology

    Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility

    Dao-Lai Zhang et al.
    ADGRG2, an orphan GPCR, when coupled to CFTR via a regional Gq signaling on the apical membrane, acts to regulate efferent duct fluid reabsorption making it essential for male fertility.
    1. Developmental Biology
    2. Neuroscience

    Identification of compounds that rescue otic and myelination defects in the zebrafish adgrg6 (gpr126) mutant

    Elvira Diamantopoulou et al.
    Results of a zebrafish whole-animal chemical screen for compounds that can rescue ear and myelination defects in an adhesion GPCR (Adgrg6/Gpr126) mutant.
    1. Cancer Biology
    2. Cell Biology

    GPCR signaling inhibits mTORC1 via PKA phosphorylation of Raptor

    Jenna L Jewell et al.
    Protein kinase A (PKA) phosphorylates Raptor and inhibits mammalian target of rapamycin complex 1 (mTORC1) activity.

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