CETSA® Navigate MS is a complementary targeted method that allows you to pursue target proteins where no antibodies are available for detection. Quantification is based on Mass spec and uses trace peptides as internal standards allowing for specific and robust profiling of individual or multiple proteins.
In a proof-of-concept study of the CETSA® Navigate MS, we focused on cyclin-dependent kinase 6, CDK6, a well-established onco-target protein3. A previously established CDK6 CETSA® Navigate assay, based on western blot detection, was used for benchmarking of the CETSA® Navigate MS assay. Pelago Bioscience profiled the cellular target engagement of CDK6 by the kinase inhibitor Palbociclib (Ibrance®) in K562 cells using the two formats in parallel to demonstrate that both assays reliably and efficiently can be used for evaluating cellular target engagement.
CETSA® Navigate MS is a valuable method to investigate different isoforms or to perform selectivity studies. Same as with the CETSA® Navigate method, this format can be applied for studies examining 1-10 compounds at a time in early feasibility studies, hit confirmation, lead optimization, and translational work. From the project start to the final report the expected timeline is around 8-10 weeks.
As a cellular target engagement assay that determines the level of interaction between a ligand and a target protein of interest in a physiologically relevant setting, CETSA® is perfectly suited for hit confirmation.
The aim at this stage of the drug discovery and development process is to optimize the compound properties to ensure the development of safe and effective candidate drugs (CDs) that can be dosed in healthy volunteers.
CETSA® can assess target engagement across a multitude of sample types. Established assays can easily be transferred from cell line to animal tissue, human primary cells, or patient-derived material, and thereby be used for translation all the way from lab bench to patient.
Check out our library to learn more about CETSA® Navigate MS. If you have any questions or want to see how CETSA® Navigate MS can be applied to your specific project, please contact us using the form below. We will get back to you as soon as we can.
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