Summary of agonist and antagonist activities for 4-cresol tested in the gpcrMAX and orphanMax panels of known and orphan G protein-coupled receptors (GPCRs), respectively.
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posted on 2024-10-24, 18:00 authored by François Brial, Géraldine Puel, Laurine Gonzalez, Jules Russick, Daniel Auld, Mark Lathrop, Roseline Poirier, Fumihiko Matsuda, Dominique GauguierThe effects were tested at at concentration of 10μM of 4-cresol. The known GPCRs were tested in both agonist and antagonist assay modes, whereas the orphan GPCRs were tested antagonist assay moce. The measured effects (%) correpond to the percentage of remaining activity for the agonist assay and the percentage of inhibition for the antagonist assay.
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screening large panelsrat pancreatic isletsmouse c2c12 myoblastskinase strongly expressedisolated rat isletsfunctional studies revealed44 pharmacological compounds241 g proteininsulin secretion inducedenhanced insulin releasetype 2 diabeteshuman primary adipocytesdiv >< pcresol dose involvesdeteriorate insulin sensitivityinsulin sensitivityvivo target effectsrsk2 ),results providepreclinical modelsmodest improvementlow doseslow concentrationsislet expressionhealth improvementglycemic controlfasting glycemiacresol dosescoupled receptorscell proliferationbody weightadditive effect
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