GPR75 has emerges as a potential metabolic disease target, but inconsistent ligand activity reports have hindered progress. At Sygnature Discovery, we have developed a suite of functional, cell-based assays to characterize GPR75 signaling and identify modulators with confidence.<\/p>\n
Using inducible HEK cell systems, we demonstrated constitutive activity through CRE reporter and \u03b2-arrestin recruitment assays, revealing inverse relationships between cAMP and \u03b2-arrestin signals. Orthogonal readouts, including G-protein dissociation and HiBiT-tagged surface expression, confirmed coupling preferences towards G\u03b1i3 and G\u03b1q pathways. These assays were optimized for high-throughput screening in 96- and 384-well formats, achieving strong assay windows and reproducible Z-factors, providing a robust platform to support agonist, inverse-agonist, and bias discovery for this orphan receptor.<\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":21737,"template":"","category":[681,709,705,747,754,753,687,688],"class_list":["post-4225","poster","type-poster","status-publish","has-post-thumbnail","hentry","category-bioscience","category-cell-based-assays","category-cell-line-generation","category-gpcrs","category-metabolic-disease","category-neuroscience","category-target-classes","category-therapeutic-areas"],"acf":[],"yoast_head":"\n