PROTAC is composed of 3 independent parts, and each part can be replaced or adjusted individually, so that there is a difference in activity between different PROTAC compounds. For example, the change of linker length has a certain effect on the activity of PROTAC to degrade the estrogen receptor. In addition, the peptide length of E3 ligase recognition motif and the binding site of the linker also changes the activity of PROTAC. The activity of PROTAC directly affects its potency and the degradation of the target protein, so it is necessary to perform PROTAC activity assay during its development and screening process.
