Like a fish out of water proteins out of the cells are not in their natural environment and their behaviour will be compromised.
Exploring your proteins out of the cell?
So, is your compound really therapeutic?
– CETSA can tell.
This is CETSA®
Thermal shift assays (TSAs) are a well-established techniques for measuring ligand binding to purified proteins. They involve subjecting the protein to varying temperatures and quantifying its thermal denaturation. The key principle is that when a ligand is bound to a protein, the melting is altered, which is known as a ‘thermal shift’ and can be used to quantify the affinity of the ligand-protein interaction.
”Perhaps the most important unique benefit of using CETSA® during lead generation is that it allows you to directly discard false positives, allowing you to fail faster and prioritize only the very best compounds”
Stina Lundgren, Drug Discovery Expert
CETSA® (Cellular Thermal Shift Assay) is based on this fundamental principle but leverages the novel insight that the melt curves can be generated in intact cells and tissues.
Adopting CETSA early can reduce your project timeline by 6-12 months and expedite the progress of projects from lead generation into the lead optimization stage.
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