RIP1‐CRE‐luc Reporter Plasmid

Background:

G-protein-coupled receptors (GPCRs) constitute the largest class of cell surface receptors. GPCR genes account for 5% of the human genome. GPCRs also represent the largest and among the most efficacious classes of therapeutic targets for diseases including cardiovascular disease, cancer, and asthma. 

Technology Overview: 

The novel cyclic adenosine monophosphate (cAMP)-responsive luciferase  reporter exhibits optimal performance in high-throughput screens of agonist binding at GPCRs. This reporter exhibits substantially reduced basal activity, a feature that is likely to be of particular importance when performing high-throughput screens in which false-positive hits are to be avoided. Compared to other reporters, the present construct affords a much wider dynamic range of activation (>340 fold-stimulation) upon exposure to GPCR agonists with cAMP signaling properties.

 Advantages:

• Significantly reduced basal luciferase activity inherent to similar reporters.
• Wide dynamic range of activation upon exposure to agonist.

 

 Applications:

• Research tool
• Drug candidate high-throughput screening