ICE Bioscience Posters

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G protein-coupled receptors (GPCRS) are the largest family of cell surface receptors (~800 members in humans). It can be activated by various stimuli and couple with different G proteins to initiate multiple signaling pathways. Dysregulation of GPCR is related to a variety of human diseases and disorders, such as metabolic diseases, cardiovascular diseases, hypertension, including cancer initiation and development.

This research established the biophysical binding platform. MegaR-engineered GPCR protein was purified for Spectral Shift technology, one of the approaches possible using the Dianthus, and Surface Plasmon Resonance assay, which is the "gold standard" for detecting interaction between ligand and targets. Furthermore, over 170 GPCRs stable cell lines were constructed for multiple assays establishment to promote GPCR drug discovery and screening. The cell-based functional assays like HTRF cAMP assay, ADCC reporter assay and β-arrestin2 recruitment are suitable for agonist, antagonist and inverse agonist validation. Consequently, the GPCR platform offers a comprehensive screening cascade for the assessment of compounds, thereby supporting diverse methodologies that are instrumental in advancing the discovery of novel anti-cancer therapeutics.