Discover Molecular Glue & PROTAC® Targets

Comprehensive validation services for Molecular Glue & PROTAC drug discovery using advanced degradation technologies

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PROTACs (PROteolysis TArgeting Chimeras) are heterobifunctional molecules with a distinct ligand that targets a specific E3 ligase which is tethered by another ligand specific for the target protein, using an optimized chemical linker. This allows for exploitation of the cell’s own degradation machinery (ubiquitin proteasome system) to degrade target proteins.

Validation of a novel target’s ability to degrade with subsequent observation of the predicted phenotype is crucial for PROTAC drug discovery.

Our Approach

At LifeSensors, we offer a comprehensive overview of endogenous target protein expression, generate cell lines with a degrader tag (dTAG, BromoTAG®) on the target protein of interest and induce selective degradation with TAGged protein of interest that can elucidate the role of the target in physiological function or a disease mechanism to produce a relevant phenotype.

Successful validation of a target followed by the design of chemical modulators like PROTACs that can selectively modulate the endogenous target is largely considered direct evidence of TPD campaign.

The in vitro ubiquitination platform was designed to monitor multiple variants of PROTAC with variable linkerology, exit vectors, variable ligands for an E3 ligase, or targets to evaluate the best combination that results in robust ubiquitination. We offer collaboration with chemistry teams to rationally design PROTACs that have superior ubiquitination efficiency that can translate into superior degradation in vivo.