Cisbio introduces GPCR-based target assay

By Wai Lang Chu

- Last updated on GMT

Related tags Signal transduction

Cisbio has introduced its second IP-One assay, which can be used by
all laboratories focused on GPCR-based targets of which 45 per cent
of currently marketed drugs owe their efficacy to.

Despite their obvious success as targets, GPCR drug discovery has remained a relatively inefficient process, typically relying on high-throughput screening of large diverse libraries.

G-protein-coupled receptors (GPCRs) are valuable molecular targets for drug discovery. An important aspect of the early drug discovery process is the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates.

Several functional assay kits based on fluorescence and/or chemiluminescence detection are commercially available for screen development.

In addition, new GPCR biosensors and high-content imaging technologies have recently been developed that hold promise for the development of functional GPCR screens in living cells.

Cisbio's offering complements Cisbio's existing IP-One HTRF assay to create a portfolio of fundamental assays for IP1 (inositol(1)phosphate) quantification and GPCR screening accessible to all laboratories.

IP-One ELISA is a monoclonal antibody-based assay that can easily detect IP1, one of the major products of the phosphatidyl inositol cascade, which tightly correlates with Gq-coupled activity.

IP-One ELISA delivers second messenger measurement and represents a way of precisely investigating molecular events occurring at the membrane level.

"Cisbio international continues its commitment to R&D innovation in the field of GPCR screening, and IP-One ELISA is yet another example of this initiative,"​ said François Degorce, head of HTRF marketing & business development, Cisbio international.

"It was important for us to enable a larger customer base, whose resources might not allow for investment in compatible laboratory equipment, to also benefit from IP-One technology."

The IP-One ELISA kit contains all the components necessary to perform 96 or 480 tests, and is able to measure small levels of IP1 concentration. Performance wise, IP-

One ELISA is rapid, sensitive (EC50: 150 nM, detection limit is 10 nM), and there is no cross-reactivity with 50 µM myo-inositol, PIP2, IP2, IP3, IP4 or PIP3.

Cells are plated in the appropriate cell culture plate and stimulated by a drug of interest; then, after lysis, the supernatant is transferred into the ELISA plate and the IP1 produced is detected by addition of the ELISA reagents.

Over 50 GPCR targets have already been validated with Cisbio's IP-One assays, reconfirming the relevance of IP1 as a new secondary messenger of G-Protein Coupled Receptors.

For more information about Cisbio international and HTRF, log onto the company's >website.

Related topics Preclinical Research

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