G-protein-coupled receptors (GPCRs) play an incredible role in a range of functions in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third and one-half of the marketed drugs act by binding to GPCRs.
GPCRs mediate many important physiological functions and are considered to be one of the most successful therapeutic targets for a broad spectrum of diseases. The design and application of high-throughput GPCR assays are critical for early drug discovery, which allow the cost-effective screening of large compound libraries to identify novel drug candidates. Early functional GPCR assays rely primarily on the measurement of G-protein-mediated 2nd messenger. Taking advantage of the continuously deepening understanding of GPCR signal transduction, many G-protein-independent pathways are used to detect the activity of GPCRs, and may provide additional information for the functional selectivity of candidate compounds. With the combination of automated imaging systems and label-free detection systems, such assays are now suitable for high-throughput screening (HTS).
Creative Bioarray offers a comprehensive selection of binding and functional GPCR assays to meet the GPCR drug discovery research needs of both chemists and biologists.
|Assay classification||Commonly used assays||Pros|
|Receptor binding assays||Radioligand binding assay||High-throughput; less interference; agonist & antagonist in one assay|
|Fluorescent ligand binding assay||Non-radioactive; high-throughput; agonist and antagonist in one assay|
|G-protein dependent assays||GTPγS binding|
|Functional cell-free assay; discrimination between full or partial agonists, neutral antagonists, inverse agonists, allosteric regulators|
|Reporter assay||Homogenous assay; high-throughput; large signal to background window|
|cAMP assay||High-throughput; very sensitive|
|Ca2+ mobilization assay||High-throughput; functional assay for live cells; obtain agonist, antagonist and allosteric modulator in one assay|
|IP3/IP1 assay||High-throughput; functional assay for live cells; good for slow binding ligands|
|G-protein independent assays||GPCR internalization assay||Image based, high-content; functional assay for live cells; generic method for all|
|β-Arrestin recruitment assay||High-throughput; image or non-image based; functional assay for live cells; useful in biased signal detection; generic method for all GPCRs|
|Label-free whole cell assay||Label-free functional assay in live cells; summation of all cellular events|
|Receptor dimerization assay||GPCR heterodimers are considered new pharmacological targets|
An ideal assay for GPCR ligand screening should be simple, nonradioactive, robust, homogenous, and easily adapted to a microtiter plate format (96-, 384-, or 1536-well) for automation. With more than 10 years of expertise in biopharmaceuticals, Creative Bioarray offers hundreds of functional and radioligand-binding GPCR assays for high-throughput screening, molecular pharmacology and molecular profiling.