LAUSR

Functional Selectivity in Cytokine Signaling Revealed Through a Pathogenic EPO Mutation

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0 Published in 2017 at "Cell"

DOI: 10.1016/j.cell.2017.02.026

Abstract: Cytokines are classically thought to stimulate downstream signaling pathways through monotonic activation of receptors. We describe a severe anemia resulting from a homozygous mutation (R150Q) in the cytokine erythropoietin (EPO). Surprisingly, the EPO R150Q mutant… read more here.

Keywords: cytokine; functional selectivity; epo; selectivity cytokine ... See more keywords

Gs- versus Golf-dependent functional selectivity mediated by the dopamine D1 receptor

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0 Published in 2017 at "Nature Communications"

DOI: 10.1038/s41467-017-02606-w

Abstract: The two highly homologous subtypes of stimulatory G proteins Gαs (Gs) and Gαolf (Golf) display contrasting expression patterns in the brain. Golf is predominant in the striatum, while Gs is predominant in the cortex. Yet,… read more here.

Keywords: golf; dependent functional; functional selectivity; dopamine receptor ... See more keywords

Functional selectivity profiling of the angiotensin II type 1 receptor using pathway-wide BRET signaling sensors

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0 Published in 2018 at "Science Signaling"

DOI: 10.1126/scisignal.aat1631

Abstract: Bioluminescence-based biosensors enable comprehensive profiling of G protein–coupled receptor signaling bias. Biosensors for GPCR-biased signaling Upon binding to ligands, G protein–coupled receptors (GPCRs) stimulate heterotrimeric G proteins and recruit β-arrestin, which dampens signaling through G… read more here.

Keywords: protein; type receptor; bret biosensors; functional selectivity ... See more keywords

Functional selectivity of EM-2 analogs at the mu-opioid receptor

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2 Published in 2023 at "Frontiers in Pharmacology"

DOI: 10.3389/fphar.2023.1133961

Abstract: The mu opioid receptor agonists are the most efficacious pain controlling agents but their use is accompanied by severe side effects. More recent developments indicate that some ligands can differentially activate receptor downstream pathways, possibly… read more here.

Keywords: interaction; analogs opioid; opioid receptor; receptor ... See more keywords

Functional Selectivity of Dopamine D1 Receptor Signaling: Retrospect and Prospect

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0 Published in 2021 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms222111914

Abstract: Research progress on dopamine D1 receptors indicates that signaling no longer is limited to G protein-dependent cyclic adenosine monophosphate phosphorylation but also includes G protein-independent β-arrestin-related mitogen-activated protein kinase activation, regulation of ion channels, phospholipase… read more here.

Keywords: selectivity dopamine; receptor signaling; selectivity; functional selectivity ... See more keywords