recently, we published a proof-of-principle study describing the implementation of thermal shift assays in a cellular format, which we call the cellular thermal shift assay (cetsa). the method allows studies of target engagement of drug candidates in a cellular context, herein exemplified with ...
we published a proof-of-principle study describing the implementation of thermal shift assays in a cellular format, which we call the cellular thermal shift
The cellular thermal shift assay (CETSA) is an attractive method of screening for protein binding molecules due to its ability to detect intracellular binding while avoiding the need to purify the protein in question. Here, the CETSA was carried out using the known BACE1 inhibitor verubecestat, ...
The cellular thermal shift assay (CETSA), as a method to determine protein–ligand interaction and cellular protein modification, has rapidly become routine laboratory practice. However, current options to determine that (1) sample was loaded in each lane of the analysed western blot and (2) the...
Recently, we published a proof-of-principle study describing the implementation of thermal shift assays in a cellular format, which we call the cellular thermal shift assay (CETSA). The method allows studies of target engagement of drug candidates in a cellular context, herein exemplified with ...
in cells should be also assessed, especially for drugs aimed at modulating intracellular signaling pathways . as a result, the development of a cellular thermal shift assay (cetsa) has become an important tool for determining the binding affinity of drugs to their intracellular targets. cell lines...
(.pdb)withaccessioncode4KIT.SupplementaryMaterials.sciencemag/cgi/content/full/science.1237515/DC1MaterialsandMethodsFigs.S1toS10TablesS1andS2References(22–31)7March2013;accepted9May2013Publishedonline23May2013;10.1126/science.1237515MonitoringDrugTargetEngagementinCellsandTissuesUsingtheCellularThermalShiftAssay...
Different from these focused phenotypic screening approaches, the cellular thermal shift assay (CETSA; Molina et al., 2013) in combination with mass spectrometry can be applied to directly monitor target binding and downstream effects on a global proteomic scale. Using CETSA mass spectrometry followed...
Moreover, cellular thermal shift assay (CETSA) experiments based on the biophysical principle of ligand-induced thermal stabilization of potential target proteins were conducted. The results showed that as the temperature gradually increased from 48°C to 66°C, PS VII intervention significantly ...
clinical resistance to this drug has been well recognized and the mechanism of this phenomenon is incompletely understood. Using the cellular thermal shift assay (CETSA), we measured the Crizotinib—ALK binding in a panel of ALK+cell lines, and correlated the findings with the ALK structure and ...