Assay development for GPCR-Gq screening

Edited by the Laboratorytalk editorial team Jun 8, 2005

Homogeneous screening platform delivers precise and time-sensitive second messenger measurement, and also represents a novel functional means of precisely investigating GPCR mechanistics

Cisbio international, a developer of HTRF technology and services used in assay development and drug screening, announced the release of its novel and homogeneous assay for use in high-throughput drug screening applications, the IP-One assay system.

The new assay development tool can be used by Cisbio's current customers who are employing the company's proprietary HTRF assay development technology and who are targeting GPCR-based targets, as well as new customers who seek a customised drug development solution that targets their specific development needs.

Cisbio's IP-One assay represents a homogeneous screening platform that delivers precise and time-sensitive second messenger measurement, and also represents a novel functional means of precisely investigating GPCR mechanistics occurring at the membrane level.

Cisbio says IP-One, which is based on its proprietary HTRF technology, is the first high throughput system that can easily detect inositol(1)phosphate (IP1), one of the major products of the phosphatidyl inositol cascade, which tightly correlates with Gq-coupled activity.

IP-One assay speeds research time and enables drug developers to focus on usable, or 'druggable' targets while reducing operational costs and staffing time.

In addition, for Cisbio's existing customers that currently deploy HTRF assays, there is a seamless transition to running the IP-One assay that involves no further capital investment in equipment or technologies.

IP-One is also compatible to a diversity of natural and chimeric constructs (eg endogeneous Gq, chimeric Ga16 coupling) that can be expressed in various cell lines.

"Cisbio has consistently proven its commitment to developing critical new assay development technologies for its customers and with our IP-One Assay, we have expanded our capabilities to provide a strategic tool that broadens our customers' drug development capabilities, specifically in the targeting of GPCRs" said Francois Degorce, head of HTRF marketing and business development, Cisbio international.

"GPCRs are the most important target class investigated in the drug discovery process and the integration of our IP-One assay and Cisbio's proprietary HTRF technology allows customers to screen these targets with a high degree of reliability.

"Concurrently, the high pharmacological relevance of the assay produces fine lead characterisation and optimisation that are much sought-after in secondary screening operations or in GPCR mechanistic studies".

The IP-One Assay integrates and combines Cisbio's proprietary HTRF technology, and is also complementary to the company's cAMP (Cyclic AMP) assay kit, allowing for the screening of GPCRs in a high throughput mode, a capability which the company says is unmatched by other technologies.

This HTRF technology-based assay is homogenous, non-radioactive, and well adapted to HTS and to miniaturisation.

Additionally, IP-One was designed on the same template as cAMP, producing a comprehensive technological platform for Cisbio's proprietary GPCR screening process.

With the addition of the IP-One assay, Cisbio now offers a complete assay development infrastructure for GPCR screening.