Inhibition of Subsets of G Protein-coupled Receptors by Empty Mutants of G Protein α Subunits in Go, G11, and G16 [PDF]
We previously reported that the xanthine nucleotide binding Goα mutant, GoαX, inhibited the activation of Gi-coupled receptors. We constructed similar mutations in G11α and G16α and characterized their nucleotide binding and receptor interaction.
Gu, Lingjie, Simon, Melvin I., Yu, Bo
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Role of G-protein coupled receptors in cardiovascular diseases
Cardiovascular diseases (CVDs) are the leading cause of death globally, with CVDs accounting for nearly 30% of deaths worldwide each year. G-protein-coupled receptors (GPCRs) are the most prominent family of receptors on the cell surface, and play an ...
Yuanqiang Li +4 more
doaj +1 more source
Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]
G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L. +1 more
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Presynaptic G Protein-Coupled Receptors: Gatekeepers of Addiction?
Drug abuse and addiction cause widespread social and public health problems, and the neurobiology underlying drug actions and drug use and abuse is an area of intensive research.
Kari A Johnson, David M Lovinger
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Current applications of mini G proteins to study the structure and function of G protein-coupled receptors [PDF]
G protein-coupled receptors (GPCRs) regulate intracellular signalling pathways that contribute to virtually all aspects of cell function. Characterising GPCRs in each of their conformational states is key to understanding their mechanism of action, but ...
Carpenter, Byron
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A modeling strategy for G-protein coupled receptors
Cell responses can be triggered via G-protein coupled receptors (GPCRs) that interact with small molecules, peptides or proteins and transmit the signal over the membrane via structural changes to activate intracellular pathways.
Anna Kahler, Heinrich Sticht
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Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio +4 more
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G-Protein coupled receptors: answers from simulations
Molecular-dynamics (MD) simulations are playing an increasingly important role in research into the modes of action of G-protein coupled receptors (GPCRs).
Timothy Clark
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Regulating G protein-coupled receptors by topological inversion
G protein-coupled receptors (GPCRs) are a family of proteins containing seven transmembrane helices, with the N- and C-terminus of the protein located at the extracellular space and cytosol, respectively.
Bray Denard +4 more
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Mas-related G-protein–coupled receptors inhibit pathological pain in mice [PDF]
An important objective of pain research is to identify novel drug targets for the treatment of pathological persistent pain states, such as inflammatory and neuropathic pain.
Altier +49 more
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