Cellular Thermal Shift Assay (CETSA®)
Target Engagement Using CETSA®: A Synergy of Our Biophysicists and Pelago Bioscience
Our biophysicists can incorporate the use of the Cellular Thermal Shift Assay platform into your integrated project via our alliance with Pelago Bioscience. The CETSA® platform provides a label free physiologically relevant measure of affinity allowing the demonstration of direct target engagement. Pelago Bioscience, founded by the inventor of CETSA® platform, is the industry leader in the application of the CETSA® to study target engagement.
CETSA® involves heating cell lysates to different temperatures and quantifying the presence of target protein in the soluble fraction by western blotting or mass spectrometry. It is suitable for studying target engagement in lysates, intact cells and tissue and is applicable to a wide range of soluble intracellular and extracellular drug targets, capable of resolving potencies from mM to fM.
A typical protein melting curve generated by Cellular Thermal Shift Assay analysis in order to study protein-ligand interactions
- Quantitative measure of target engagement
- Physiologically relevant readout of affinity
- Suitable for lysates, intact cells and tissue
- Applicable to a wide range of soluble intracellular and extracellular drug targets as well as membrane protein targets
- Monitor target specificity, drug transport and activation
- Label free