Jul 1, 2016 · The direct measurement of drug-protein interactions in living cells is a major challenge in drug discovery research. Using the cellular thermal shift assay or CETSA such measurements can be achieved, in principle, in any cell samples and in microtiter-plate format.

CEllular Thermal Shift Assay (CETSA®) is a patented label free chemoproteomics method that has enabled measurements of compound target engagement in intact cells and tissue, without modifications to the target protein.

Aug 7, 2014 · The cellular thermal shift assay–CETSA–exploits this to characterize intracellular drug-protein engagement. Thermal shift assays are used to study thermal stabilization of proteins upon...

The CETSA protocol consists of four key steps: compound incubation with live cells or lysates, heat treatment at different temperatures, separation of proteins that remain folded from the ones that have denatured, and finally the protein detection step.

Jul 5, 2013 · We have developed a method for evaluating drug binding to target proteins in cells and tissue samples. This cellular thermal shift assay (CETSA) is based on the biophysical principle of ligand-induced thermal stabilization of target proteins.

CETSA is a biophysical assay based on the principle of ligand-induced thermal stabilization of target proteins, meaning that a proteins melting temperature will change upon ligand interaction.

Jul 5, 2013 · We have developed a method for evaluating drug binding to target proteins in cells and tissue samples. This cellular thermal shift assay (CETSA) is based on the biophysical principle of ligand-induced thermal stabilization of target proteins.

Jan 1, 2020 · The Cellular Thermal Shift Assay (CETSA®) is well suited for identifying target engagement between ligands and their protein targets. Several studies have shown that CETSA combined with MS is a powerful technique that allows unlabeled target deconvolution in complex samples such as intact cells and tissues in addition to cell lysates and other ...

Here, we present the development and validation of a homogeneous, standardized, target-independent, and high-throughput (384- and 1536-well formats) CETSA platform that uses a split Nano Luciferase approach (SplitLuc CETSA).

Feb 8, 2025 · Cellular Thermal Shift Assay (CETSA) is a valuable technique for studying protein stability and interactions within cells. It plays a crucial role in drug discovery by validating potential drug targets through the observation of protein denaturation under varying thermal conditions.