Automating GPCR Functional Assays in Collaboration With Cisbio International

G protein-coupled receptors (GPCRs) are transmembrane proteins on a cell's surface that can interact with the environment both outside and inside the cell [1]. More than 50% of currently marketed drugs target GPCRs. Within cells, GPCRs carry information via two major signaling pathways: regulation of cAMP levels and increases in intracellular Ca2+ triggered by inositol (1, 4, 5) tri-phosphate (IP3) [2].

Cisbio developed a highly accurate homogenous time-resolved fluorescence (HTRF®) assay for measuring IP1, a downstream metabolite of IP3, which accumulates in cells following Gq recepetor activation and is stable in the presence of LiCl, making it an ideal GPCR (Gq) functional assay.

Beckman Coulter offers versatile liquid handlers, microfluidic workstations, and a high-end multimode reader, serving a full spectrum of drug discovery applications. Recently, Cisbio International has awarded its (HTRF) certification to PARADIGM™ Detection Platform, made by Beckman Coulter, the first user-upgradeable and -configurable multimode reader.
In collaboration with Cisbio International, Beckman Coulter has automated an array of GPCR functional assays including the IP-One HTRF assay and cAMP cell-based assays with detection and analysis using Biomek® NXP Workstation, BioRAPTR FRD™ Microfluidic Workstation and PARADIGM Detection Platform, made by Beckman Coulter.

In addition, Beckman Coulter and Cisbio released joint scientific presentations and publications demonstrating the applications of the validated automation methods for GPCRs in drug discovery at Lab Automation 2008, January 27–30, Palm Springs, CA and The Society for Biomolecular Sciences (SBS) 14th Annual Conference & Exhibition, St. Louis, Mo., April 6-10, 2008. The combined offering in automating Cisbo’s GPCR cell-based assays will continue to enable and drive the advancement in cell-based drug screening process.