Dr. GPCR Summit 2021
- Dr. Sonia Martínez Arca -
- Celtarys Research -
- Santiago de Compostela, A Coruña, España -
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 overcoming this bottleneck making fluorescence-based techniques a real option in drug discovery. Our USP is the fact that we can typically design and synthesize novel fluoro ligands for completely new targets, and orphan targets, in a fraction of the usual time, thanks to our patented synthesis technology.
We have initially applied our technology to GPCRs, generating fluorescent GPCR probes with outstanding binding and selectivity characteristics, that have been externally validated in several HTS assays (FRET, HCS, Flow cytometry, Fluorescence Polarization…). We count with more than 20 validated fluorescent ligands for several GPCR families such as Dopamine, Serotonin, Adenosine, and Cannabinoids. These fluorescent GPCR ligands can be potent tools for GPCR drug discovery, positioning Celtarys as a game changer technology in the sector.
Sonia Martínez Arca, Celtarys Research
Maria Majellaro, Celtarys Research
Eddy Sotelo, Celtarys Research and University of Santiago de Compostela
Gonzalo Pazos, Celtarys Research