GPCR Stable Cell Lines
GPCR (G Protein-Coupled Receptor) stable cell lines are engineered cell lines that stably express a specific GPCR. GPCRs represent one of the largest families of membrane proteins involved in various physiological processes and are major drug targets in therapeutic research. These stable cell lines are widely used to study receptor-ligand interactions, signaling pathways, and drug screening.
Content on GPCR Stable Cell Lines
- Generation:
- Vector Design: A plasmid containing the GPCR gene is designed with a strong promoter (e.g., CMV, EF1α) and a selection marker (e.g., hygromycin or neomycin resistance).
- Host Cells: Common host cells include HEK293, CHO, or U2OS due to their compatibility with GPCR expression.
- Characteristics:
- Stable Integration: The GPCR gene is integrated into the host genome for consistent expression.
- Receptor Functionality: Retains functional activity, including ligand binding, G-protein coupling, and signal transduction.
Applications of GPCR Stable Cell Lines
- Drug Discovery and Development:
- High-throughput screening (HTS) of GPCR-targeted drugs, such as agonists, antagonists, or allosteric modulators.
- Optimization of drug efficacy and safety profiles using functional assays.
- Signaling Pathway Studies:
- Enable detailed investigation of GPCR-mediated signaling cascades, such as cAMP, IP3, or MAPK pathways.
- Help elucidate GPCR coupling with G-proteins or β-arrestins.
- Toxicology Studies:
- Assess potential off-target effects of drugs on GPCR signaling and cellular health.
GPCR stable cell lines are invaluable tools in both basic research and drug discovery, providing a reliable and scalable system to study one of the most pharmacologically significant protein families.
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