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Speeding up drug discovery and development with fluorescent biosensors technology

Country of Origin: Spain
Reference Number: TOES20210409003
Publication Date: 23 April 2021

Summary

A Basque biotechnology SME provider of cell-based assays for drug discovery & development applications 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 High-Throughput Screening (HTS) and High-Content Screening (HCS) platforms. They are looking for commercial with technical assistance or licence agreements.

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 (HTS) and High-Content Screening (HCS) in drug discovery. 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 and development programs.
The SME has developed a novel family of genetically encoded fluorescent biosensors, expressed in human stable cell lines, for measuring G-protein coupled receptors (GPCR) activity in living cells by means of analysing 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 mechanisms and kinetics of GPCR activation.
This family of biosensors has been developed to measure changes in second messengers (Ca2+, cAMP or DAG) and β-arrestin signaling pathways. Upon activation, the biosensors undergo a structural folding that promotes their relocation in the vesicular trafficking and a subsequent increase in the total fluorescence intensity inside the cells. These changes can be easily quantified by fluorescent emission in a plate reader or by image analysis with an automated microscopy system.
The activation of a GPCR triggers an important cellular response that involves changes in the concentration of second messengers such as Ca2+, cAMP or DAG and the subsequent receptor´s recruitment through β-arrestin protein family.
Actually, the company has developed different families of biosensors depending on the signaling pathway of interest. All of them are available with the green fluorescent protein turboGFP and/or red fluorescent protein turboFP650. These biosensors can also be combined in the same cell line to perform multiplex assays.
Currently, 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.
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Advantages and Innovations

This technology allows the performance of drug discovery screening campaigns measuring second messengers and β-arrestin concentration changes simultaneously in living cells. The technology can be applied to study GPCRs activation/inhibition, to identify the signaling pathways of orphan receptors, to perform functional assays, to discover biased ligands or to characterize new GPCR ligands that can become potential new drugs.

The main advantages are:
• Simple integration of the technology in HTS or HCS screening campaigns.
• Performance of multiplex assays combining the different families of the fluorescent biosensors.
• Non-tagged GPCRs.
• Economic and easy to use assay. No additional reagents required to perform the determinations.

These technology assays are extremely robust and well suited for screening applications. The use of these biosensors in a screening campaign enables a reduction of up to 50-70% of the time, costs and resources neccessary.

Stage Of Development

Already on the market

Requested partner

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) and high-content screening (HCS) applications.

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