"In the drug discovery process gold standard techniques have relied on radioactivity for identifying and characterizing new drug candidates. In the last years, due to radioactivity stringent requirements, high costs and environmental concerns, fluorescence-based assays started to be used. However, fluorescent ligand employment has not been adopted widely due to the challenging chemical development process and the consequent lack of optimal fluorescent probes available for the majority of the therapeutical targets. Our technology allows to overcome this bottleneck making fluorescence-based techniques a real option in drug discovery.
Celtarys Research has developed a highly versatile conjugation methodology for the efficient optimization of fluorescent probes for drug discovery. We can develop fluorescent ligands in a timely manner with optimal pharmacological and photophysical properties for any target with therapeutic interest outperforming radioligands and other available fluorescent probes, thus improving drug discovery. The relevant role of GPCRs in drug discovery led us to start applying our technology for these targets, developing fluorescent probes for different receptor families and applications. We have developed >20 GPCR fluorescent ligands for Adenosine, Serotonin, Dopamine and Cannabinoid receptors. Celtarys fluorescent probes have been validated in a variety of High Throughput Screening (HTS) assays, including HTRF-based assays, High Content Screening, Fluorescence Polarization, Flow Cytometry and Fluorescence Microscopy. Celtarys probes have been successfully used in transfected and native cells and its validation has been conducted both in house and in collaboration with distinct European research groups expert in the different HTS assays.
The fluorescent probes obtained applying our technology are built upon a pharmacophore representative of the target, show high affinity (Ki < 100 nM) and selectivity and are engineered with ad-hoc spacers tuned to allow target recognition; moreover, their fluorophores are stable, guarantee the affinity for the target and display a variety of photo-physical properties meeting market demands.
Further to our catalogue, our technology, together with our expertise in Medicinal Chemistry, Chemical Biology, Photophysical methods, Pharmacology and HTS, enables us to develop in a competitive manner and short time ( < 3 months) personalized fluorescent ligands with optimal pharmacological and photophysical properties for any target of interest. The application of our proprietary Lego-like conjugation approach to other important target families (e.g., Kinases and nuclear receptors) is currently in progress, thus validating the scope of Celtarys technology with novel tailored fluorescent probes.
In summary, we have a solution to the present barriers that prevent an effective deployment of fluoresce-based techniques in drug discovery: our efficient and versatile semi-combinatorial conjugation strategy that enables the ad-hoc generation of optimal fluorescent ligands for diverse targets in a time and cost-effective manner. Celtarys technology emerges as a game-changing technology destined to revolutionize and accelerate fluorescence-based methods in drug discovery.
At Celtarys Research we believe that our innovation fits within SLAS’s area of life science because we propose a technological advance that will help to improve the performance of the early phases of drug discovery, through the offer to the scientific community of innovative fluorescent ligands suitable for High Throughput Screening (HTS) assays, outperforming radioligands and other available fluorescent probes."