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Synthetic GPCRs for controlling cellular responses.
Nat Biotechnol
January 2025
Nature Biotechnology, .
Development of a yeast-based sensor platform for evaluation of ligands recognized by the human Free Fatty Acid 2 Receptor.
FEMS Yeast Res
January 2025
Department of Life Sciences, Chalmers University of Technology, 412 58 Gothenburg, Sweden.
Yeast-based sensors have shown great applicability for deorphanization of G protein-coupled receptors (GPCRs) and screening of ligands targeting these. A GPCR of great interest is free fatty acid 2 receptor (FFA2R), for which short-chain fatty acids such as propionate and acetate are agonists. FFA2R regulates a wide array of downstream receptor signaling pathways in both adipose tissue and immune cells and has been recognized as a promising therapeutic target, having been implicated in several metabolic and inflammatory diseases.
View Article and Find Full Text PDFAutomated Plate Reader-Based Assays of Light-Activated GPCRs.
Methods Mol Biol
December 2024
Australian Regenerative Medicine Institute (ARMI), Faculty of Medicine, Nursing and Health Sciences, Monash University, Clayton, VIC, Australia.
In the emerging field of optogenetics, light-sensitive G-protein coupled receptors (GPCRs) allow for the temporally precise control of canonical cell signaling pathways. Expressing, stimulating, and measuring the activity of light-sensitive GPCRs (e.g.
View Article and Find Full Text PDFDevelopment of a Class A/B Hybrid GPCR System for the Proximity-Assisted Screening of GPCR Ligands.
ACS Chem Biol
January 2025
Department Chemistry and Biochemistry Clemens-Schöpf-Institute, Technical University Darmstadt, Peter-Grünberg Straße 4, Darmstadt 64287, Germany.
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, which is especially critical for poorly druggable GPCRs. Here, we present a proximity-based screening system for class A GPCRs, which adopts the natural two-step activation mechanism of class B GPCRs.
View Article and Find Full Text PDFActivation of the Melatonin Receptor MT by the Natural Product Gastrodin to Promote Sleep.
J Pineal Res
November 2024
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, People's Republic of China.
The activation of melatonin receptors, belonging to the G-protein coupled receptors (GPCRs) superfamily, has been recognized as a vital approach in the clinical management of sleep disorders. Although the natural agonist melatonin and synthetic agonists (e.g.
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