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Identification of Small Molecule Drug Targets Based on Thermal Proteome Profiling

Background Information

Cellular Thermal Shift Assay (CETSA) is an experiment that assesses the binding efficiency of drugs and target proteins.As the temperature increases, proteins will undergo denaturation, structural changes, and even aggregation. Once  a protein binds to its corresponding ligand, a small molecule drug, the thermal stability of this protein will change. Therefore, the detection of protein thermal stability can be used to evaluate their interactions.

Technical Platform

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Our Advantages

1. No need to modify the target small molecules, avoid changes in structure-activity relationships, and simplify experimental design.
2. Applicable to pure proteins, Iysates (cells or tissues, etc.)
3. Reflect direct interactions between proteins and small molecules.

Case Study

Project Aim: Verify whether the target small molecule is directly bound to the target protein in cell lysate through TPP.

Solutions: Analyze the thermal stability of the target protein using Western blotting (Figure 1), temperature range TPP-TR (Figure 2)and compound concentration range TPP-CCR (Figure 3).

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