ADVANCING PROTEIN DEGRADERS PROTACS or MOLECULAR GLUES

ü  Mass spectrometry driven measurements, uniquely tailored for the development of PROTACs.

ü  Cell uptake studies – Incubation of PROTACs with specific cell lines and evaluation of cell uptake. Similar approaches for tissue uptake studies following PROTAC administration provide the path for in vivo studies.

ü  Protein (POI target) ablation studies by MS: Incubation of PROTACs with cancer cell lines to determine the ablation of POI by LC-MRM.  A technique developed by our group with significant advantages over western blot (WB) assays or the more recently developed HiBiT degradation assays (details available upon request).

ü  Pharmacokinetics (PK) of PROTACS – unique approaches for determining the PK and bio-distribution properties in animal models.  Several examples of work performed for leading biotech companies to enhance the chances of PROTAC clinical drug development (enhancing oral bioavailability).

ü  Mechanism of action insights, provide opportunities for co-dosing schemes often required in anti-cancer therapies.