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Table 1 A comparison among different generations of PROTACs

From: Protein degradation technology: a strategic paradigm shift in drug discovery

  1st generation 2nd generation 3rd generation
Advantages Larger contact interface with POI and more choices of modification on the drug Applicable for “undruggable” targets; good cell permeability and solubility Well-controllable biological characters; causing protein degradation in a highly specific temporal and spatial manner
Disadvantages Poor cell permeability and stability [18] Potential off-target effects, relatively high molecular weight, and toxicity [18, 21, 23, 24] Potential damage to DNA by UV light and low tissue penetration [18, 27]