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Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
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Chapters
- 00:04Introduction
- 01:04Transfection of HEK293T Cells
- 02:36Incubation of Cells with SHP2 Inhibitors
- 05:11Isothermal or Thermal Profile Gradient Heat Pulse
- 06:01Results: Cellular Target Engagement of Allosteric SHP2 Inhibitors with SHP2-WT and SHP2-E76K Proteins
- 08:03Conclusion
The ability to assess target engagement by candidate inhibitors in intact cells is crucial for drug discovery. This protocol describes a 384 well format cellular thermal shift assay that reliably detects cellular target engagement of inhibitors targeting either wild-type SHP2 or its oncogenic variants.
