Partnering opportunity

Fluorescent biosensors for multiplexing G protein-coupled receptors (GPCR) functional assays

Summary

A Basque biotechnology SME focused on developing cell-based assays for High-Throughput Screening (HTS) & High- Content Analysis (HCA) has developed a family of fluorescent biosensors which allows the measurement of different G protein-coupled receptor (GPCR) activation pathways (G-Protein & β-arrestin) simultaneously in living cells by fluorescent imaging analysis on most HTS & high-content screening (HCS) platforms. They are looking for commercial with technical assistance or licence agreements

Partner sought

The company wishes to collaborate with pharmaceutical or biotechnology companies, research centres and/or government institutions interested in accelerating and improving their drug discovery programs. They are looking for a commercial agreement with technical assistance or a licensing agreement regarding the use of new fluorescent biosensors assays technology as a highly robust and well suited tool for high throughput screening (HTS) applications.

Description

The company is a dynamic and R&D intensive biotechnological SME located in the Basque Country. They are focused on developing cell-based assays for High-Throughput Screening and High-Content Analysis. They also act as a contract research organization providing drug screening services and on-demand assay development. Their goal is to accelerate and improve their customer’s drug discovery programs. This SME has developed a novel family of fluorescent biosensors for measuring G-protein coupled receptors (GPCR) activity in living cells by means of analysing the different activation pathways simultaneously. Each biosensor of the family co-expressed with a GPCR, provides an innovative and sensitive research tool for studying the molecular mechanism and kinetics of GPCR activation. These biosensors enable the measurement of both, beta-arrestin recruitment and second messenger concentration changes (Ca++, cAMP, DAG) involved in GPCR activation. An increase in the second messenger concentration leads to a change in the structural folding of the green fluorescent biosensor that increases its intensity signal. At the same time, when activated & phosphorylated GPCR binds the beta-arrestin, leads another change in the structural folding of the red fluorescent biosensor, increasing also its fluorescence intensity. Four different versions of biosensors have been actually developed: β-arrestin, cAMP, Ca++ and DAG. The company is looking for a commercial agreement with technical assistance or a licensing agreement with pharma or biotech companies, research centres or government institutions interested in accelerating and improving their drug discovery programs.

Advantages and innovations

The new biosensors technology allows for the performance of screening campaigns measuring both β-arrestin & second messenger concentration changes simultaneously in living cells by fluorescence intensity. It could be applied to GPCRs activation/inhibition studies, primary cells or to orphan receptors because this technology allows performing multiplex assays. The main advantages are: • Performance of multiplex analysis, analysing both GPCR activation pathways • Different second messenger application: cAMP, Ca++, DAG. • β-Arrestin recruitment monitorization • Direct identification of biased ligands • Non-tagged GPCRs. • Economic assay. It is not required to use additional reagents to perform the determinations. The biosensors assays are highly robust and well suited for high throughput screening (HTS) applications. The use of these biosensors in a HTS campaign reduces the time, costs and resources needed in more than a 50-70%.

Development stage

Already on the market

Intellectual Property Rights (IPR)

Patent(s) applied for but not yet granted,Patents granted


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