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   Articles with "gpcr" as a keyword



GPCR Signaling From Intracellular Membranes − A Novel Concept

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recommendations! Published in 2017 at "BioEssays"

DOI: 10.1002/bies.201700200

Abstract: The properties of the main psychoactive compound of the Cannabis plant, namely Δ-tetrahydrocannabinol (THC), have been recognized for a long time. Ever since the discovery of cannabinoid receptors (CB1R and CB2R) and the characterization of… read more here.

Keywords: intracellular membranes; gpcr signaling; concept gpcr; gpcr ... See more keywords
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GPCR Signaling Regulation in Dictyostelium Chemotaxis.

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recommendations! Published in 2021 at "Methods in molecular biology"

DOI: 10.1007/978-1-0716-1258-3_27

Abstract: GPCR signaling is the most prevailing molecular mechanism for detecting ambient signals in eukaryotes. Chemotactic cells use GPCR signaling to process chemical cues for directional migration over a broad concentration range and with high sensitivity.… read more here.

Keywords: regulation dictyostelium; signaling regulation; gpcr signaling; gpcr ... See more keywords

Co-IP assays for measuring GPCR-arrestin interactions.

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recommendations! Published in 2019 at "Methods in cell biology"

DOI: 10.1016/bs.mcb.2018.09.003

Abstract: βarrestin1 and -2 (also known as arrestin2 and -3, respectively) are G protein-coupled receptor (GPCR) adapter proteins, performing three major functions in the cell: functional desensitization, i.e., G protein uncoupling from the receptor, GPCR internalization… read more here.

Keywords: gpcr arrestin; gpcr; measuring gpcr; assays measuring ... See more keywords
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GPCR mediated control of calcium dynamics: A systems perspective

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recommendations! Published in 2020 at "Cellular Signalling"

DOI: 10.1016/j.cellsig.2020.109717

Abstract: Abstract G-protein coupled receptor (GPCR) mediated calcium (Ca2+)-signaling transduction remains crucial in designing drugs for various complex diseases including neurodegeneration, chronic heart failure as well as respiratory diseases. Although there are several reviews detailing various… read more here.

Keywords: systems perspective; control; ca2 signaling; gpcr ... See more keywords
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Integration of GPCR Signaling and Sorting from Very Early Endosomes via Opposing APPL1 Mechanisms

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recommendations! Published in 2017 at "Cell Reports"

DOI: 10.1016/j.celrep.2017.11.023

Abstract: Summary Endocytic trafficking is a critical mechanism for cells to decode complex signaling pathways, including those activated by G-protein-coupled receptors (GPCRs). Heterogeneity in the endosomal network enables GPCR activity to be spatially restricted between early… read more here.

Keywords: integration gpcr; signaling sorting; gpcr signaling; gpcr ... See more keywords

Exploring Bias in GPCR Signaling and its Implication in Drug Development: A One-Sided Affair.

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recommendations! Published in 2024 at "Biochemistry"

DOI: 10.1021/acs.biochem.4c00676

Abstract: G protein-coupled receptors (GPCRs) play a pivotal role in regulating numerous physiological processes through their interactions with two key effectors: G proteins and β-arrestins (βarrs). This makes them crucial targets for therapeutic drug development. Interestingly,… read more here.

Keywords: bias gpcr; biased signaling; drug; gpcr ... See more keywords

GPCRSPACE: A New GPCR Real Expanded Library Based on Large Language Models Architecture and Positive Sample Machine Learning Strategies.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c01983

Abstract: The quest for novel therapeutics targeting G protein-coupled receptors (GPCRs), essential in numerous physiological processes, is crucial in drug discovery. Despite the abundance of GPCR-targeting drugs, many receptors lack selective modulators, indicating a significant untapped… read more here.

Keywords: large language; machine learning; language; gpcr ... See more keywords

Development of a Class A/B Hybrid GPCR System for the Proximity-Assisted Screening of GPCR Ligands.

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recommendations! Published in 2024 at "ACS chemical biology"

DOI: 10.1021/acschembio.4c00658

Abstract: Class A G protein-coupled receptors (GPCRs) are key mediators in numerous signaling pathways and important drug targets for several diseases. A major shortcoming in GPCR ligand screening is the detection limit for weak binding molecules,… read more here.

Keywords: system; class hybrid; class; development class ... See more keywords

Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology

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recommendations! Published in 2018 at "Journal of the American Chemical Society"

DOI: 10.1021/jacs.7b11422

Abstract: Noninvasive methods to modulate G protein-coupled receptors (GPCRs) with temporal and spatial precision are in great demand. Photopharmacology uses photons to control in situ the biological properties of photoswitchable small-molecule ligands, which bodes well for… read more here.

Keywords: gpcr; antagonist toolbox; real time; photopharmacology ... See more keywords

Single-cell profiling reveals heterogeneity and functional patterning of GPCR expression in the vascular system

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recommendations! Published in 2017 at "Nature Communications"

DOI: 10.1038/ncomms15700

Abstract: G-protein-coupled receptor (GPCR) expression is extensively studied in bulk cDNA, but heterogeneity and functional patterning of GPCR expression in individual vascular cells is poorly understood. Here, we perform a microfluidic-based single-cell GPCR expression analysis in… read more here.

Keywords: single cell; gpcr; heterogeneity functional; gpcr expression ... See more keywords

Highly biased agonism for GPCR ligands via nanobody tethering

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recommendations! Published in 2024 at "Nature Communications"

DOI: 10.1038/s41467-024-49068-5

Abstract: Ligand-induced activation of G protein-coupled receptors (GPCRs) can initiate signaling through multiple distinct pathways with differing biological and physiological outcomes. There is intense interest in understanding how variation in GPCR ligand structure can be used… read more here.

Keywords: nanobody tethering; highly biased; biased agonism; gpcr ... See more keywords