A ligand or compound that binds to a G-protein coupled receptor (GPCR) may induce or inhibit multiple signaling pathways, such as activation of G proteins and β-arrestin. Furthermore, more than one G protein subtype may bind to its cognate receptor. The properties of a ligand that preferentially activate or inhibit one pathway over another are described as signaling bias and screening compounds for biased signaling may lead to selective perturbation of disease-specific pathways. Measuring compound activities in assays in the same cellular environment using unmodified GPCRs, recombinant or native, is key for accurate signaling bias analysis. Our newly developed proprietary MultiScreen™ β-arrestin technology overcomes the receptor-tagging drawback of other existing technologies, enabling high-throughput detection of β-arrestin translocation induced by native GPCRs in vitro and in vivo for the first time. This presentation will highlight these novel features and the robustness of this new assay.
- Learn how GPCR signaling bias may present opportunities for novel GPCR drug discovery.
- Discover the advantages of MultiScreen™ technology for measuring β-arrestin translocation in a native GPCR environment in high throughput.
- Discover how Multispan can uniquely empower your drug discovery efforts through our assay expertise and multiple assay platforms.
Lisa Minor, Ph.D.
Dr. Minor is a well recognized scientific expert with 25 years of experience in drug discovery encompassing several therapeutic areas, high throughput screening and safety profiling through her tenure at Johnson and Johnson Pharmaceuticals. She is an editor for the Assay Guidance Manual for NIH, served for 8 years as a member of the advisory board for the Society for Biomolecular Sciences (now Society for Laboratory Automation and Screening) and on the Scientific Advisory Board for the National Toxicology Program and chaired multiple international assay development meetings. She has been consulting for Multispan since January, 2012. Dr. Minor received her postdoctoral training at the Medical College of Pennsylvania and obtained her Ph.D. in Biological Chemistry from the Pennsylvania State University.
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