HTRF robustness and sensitivity applied to new functional cell-based assay for better understanding of complex GPCR pathways

Bagnols-sur-Cèze, France – Cisbio Bioassays (www.htrf.com), a member of IBA group and global developer of HTRF® (Homogeneous Time-Resolved Fluorescence) technology and services used in assay development and drug screening, today announced the launch of the HTRF-based Cellul’erk assay for phosphorylated-ERK1/2 investigation. This new kit for exploring G-protein Coupled Receptor (GPCR) signaling pathways is Cisbio Bioassays’ latest addition to its expanding HTRF-based platform of functional tools for GPCR and cell surface receptor investigation, major targets in drug discovery research.

Cellul’erk is a cell-based assay that directly detects endogeneous phosphorylated ERK1/2. This new, efficient functional readout for exploring GPCR signaling pathways in a high throughput mode targets ERK (extracellular signal-regulated kinase), whose phosphorylation can be modulated upon GPCR activation either through G-protein or B-Arrestin. Based on Cisbio Bioassays’ robust and sensitive HTRF technology, its straightforward assay protocol and antibody-based detection provides a simple and rapid alternative to Western blot or ELISA that is sensitive enough for endogeneous and over-expressed receptors and can be miniaturized to 1536-well formats.

“Cisbio Bioassays understands the importance of GPCR investigation and is committed to putting new tools in the hands of our customers that address the latest evolution in this area,” said François Degorce, head of marketing at Cisbio Bioassays. “Cellul’erk, which is based on the same reader and technology as the other tools in our GPCR platform, provides a new solution for studying GPCRs, and is easy for current HTRF users to implement or for new users to adopt. In parallel with Tag-lite™, which offers a more extra-cellular vision of the receptor mechanistics, this new kit reaffirms our dedication to further developing our GPCR and cell surface receptor platform.”

Cisbio Bioassays has long been at the forefront of research and development in GPCR investigation, applying HTRF to cell-based formats to create a growing number of tools that provide information about cell function and receptor activity in a high throughput mode. GPCRs, with their complex signaling network pathways, are the most important target class studied in the drug discovery industry today. They act via G-proteins to regulate a wide range of cellular functions. Upon stimulation, these receptors activate effectors that influence intracellular concentrations of second messengers such as IP1 and cAMP, and also mediate ERK1/2 phosphorylation. Following Tag-lite cell surface receptor technology and IP-One and cAMP second messenger assays, Cellul’erk marks the next step in Cisbio Bioassays’ development of mechanistic and functional tools.

Cellul’erk will be available to customers worldwide through Cisbio Bioassays’ sales force in North America and Europe and from its distributors in other areas.