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Frontiers in Cell and Developmental Biology, 2023 Introduction: G-protein coupled receptors (GPCRs) are the largest family of human receptors that transmit signals from natural ligands and pharmaceutical drugs into essentially every physiological process.
Siri Leemann, Sonja Kleinlogel
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Designer lipid-like peptides [PDF]
, 2011 A crucial bottleneck in membrane protein studies, particularly G-protein coupled receptors, is the notorious difficulty of finding an optimal detergent that can solubilize them and maintain their stability and function. Here we report rapid production of
Baaske, Philipp +11 more
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Powdered G-Protein-Coupled Receptors [PDF]
The Journal of Physical Chemistry Letters, 2016 Preparation and storage of functional membrane proteins such as G-protein-coupled receptors (GPCRs) are crucial to the processes of drug delivery and discovery. Here, we describe a method of preparing powdered GPCRs using rhodopsin as the prototype. We purified rhodopsin in CHAPS detergent with low detergent to protein ratio so the bulk of the sample ...
Suchithranga M D C, Perera +2 more
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Royal Society Open Science, 2022 Gold nanoparticles have a high potential to be a treatment of diseases by their specific drug delivery properties and multivalent receptor stimulation.
Rebecca Claßen +4 more
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G Protein–Coupled Receptor Heteromers [PDF]
Annual Review of Pharmacology and Toxicology, 2016 G protein–coupled receptors (GPCRs) compose one of the largest families of membrane proteins involved in intracellular signaling. They are involved in numerous physiological and pathological processes and are prime candidates for drug development. Over the past decade, an increasing number of studies have reported heteromerization between GPCRs.
Gomes, Ivone +5 more
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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]
, 2003 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 RECEPTOR KINASES [PDF]
Annual Review of Biochemistry, 1998 G protein–coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein–coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
J A, Pitcher +2 more
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Presynaptic G Protein-Coupled Receptors: Gatekeepers of Addiction?
Frontiers in Cellular Neuroscience, 2016 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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Role of G-protein coupled receptors in cardiovascular diseases
Frontiers in Cardiovascular Medicine, 2023 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
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Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]
, 2007 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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