Biology Section

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Post-Doctoral Fellows

  • María Elena Hernández

Technicians

  • Mª Isabel Albarrán
  • Antonio Cebriá
  • Elena Gómez-Casero
  • Javier Klett
  • Mª del Carmen Rodríguez de Miguel

Target Engagement assays measure compound binding to a selected target protein inside living cells and enable making correlations with biochemical activity. BRET or bioluminescence resonance energy transfer can be used to study cellular target engagement. NanoBRET assays are based on the fact that NanoLuc luciferase fusion proteins expressed in cells can transfer energy to a proximal fluorophore called tracer. Compound affinity to a given protein can be measured by competitive displacement of the tracer reversibly bound to the corresponding NanoLuc luciferase fusion protein in cells. In the case of PROTACs (Proteolysis Targeting Chimeras), target engagement assays are essential to evaluate the affinity of PROTACs to both the target protein and the E3 ligase, as binding to both is required for the formation of the ternary complex, which triggers the degradation of the target protein. We apply BRET assays routinely in our projects to help in the optimisation of our molecules.

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