Cellomics Cellprofiler Atto Transfluor

Gentaur Atto

Ranking of β2 Adrenergic Receptor Agonists and Antagonists

Using a Cell-Based GPCR Signaling Application

Chandrasekaran Vasudevan and Jeffrey R. Haskins


G-protein coupled receptor (GPCR) signaling has great

importance in physiological development and various biological

processes and hence has become a significant focus for various

therapeutic groups in the area of drug discovery. As many of the

various GPCR signaling pathways have been well characterized,

a large number of chemical libraries are being synthesized

targeting the various GPCRs either as agonists or antagonists.

These compounds are usually ranked for potency against a

specific GPCR based on homogeneous biochemical assays. The

β2 adrenergic receptor (β2-AR) is a member of the GPCR family

of receptors, linked to adenylyl cyclase. The activation of β2-AR

is regulated by the binding of β-arrestins to the phosphorylated

receptor, leading to the internalization of the receptor. Cellomics

Inc., has developed a cell based high content screening, GPCR

Signaling BioApplication for the ArrayScan® HCS Reader that

uses Norak’s Transfluor™ technology and allows for the screening

of compounds that affect the GPCR signaling cascade. This

application quantitates GPCR activation by measuring

translocation of a GPCR activated β2-arrestin-GFP chimera in

Transfluor® assay by iCyte™ imaging cytometer - An advanced cell based screening technology applicable to GPCRs - Kazuo Ozawa Etsuo Shinohara Sachiko Karaki Olympus Co. Genome Medical Business Division January 30, 2004 Norak Biosciences A biotechnology company based in Research Triangle Park, NC, utilizing its Transfluor® technology to become a world leader in the discovery and development of drugs that regulate G protein-coupled receptors (GPCRs). Transfluor® technology A patented, universal GPCR drug discovery technology based on the translocation of arrestin protein from cytosol to GPCR on the membrane.