in drug sensitivity studies. section 1 of this chapter describes the generation of ba/f3 clones whereas section 2 details the use of cetsa to evaluate drug binding to ror1 along with methods suitable for calculation of the binding affinity. thermal shift assays provide information about a protein...
cellular thermal shift assay
such assays have been used extensively on purified proteins in the drug discovery industry and in academia to detect interactions. 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 ...
Tan, B. X. et al. Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays.Scientific reports5, 12116 (2015). Article
Interaction between a drug and its protein target results in a shift in thermal stability of that protein. The cellular thermal shift assay–CETSA–exploits this to characterize intracellular drug-protein engagement. Thermal shift assays are used to stud
The disclosure provides methods for carrying out Real Time Cellular Thermal Shift Assays (RT-CETSA). Also provided are molecular constructs and protein constructs for use in such assays and devices suitable for carrying out such assays.
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 ...
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For protein–ligand binding in particular, this assay provides unique advantages over other thermal shift assays as engagement occurs intracellularly where additional pharmacological properties (such as ligand permeability and toxicity) may also be inferred. The CETSA essentially detects a fluctuation of a...
Assessment of the interactions between a drug and its protein target in a physiologically relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery space. The Cellular Thermal Shift Assay (CETSA) enables such an asses