PROteolysis TArgeting Chimera (PROTAC) technology is an effective tool to induce targeted degradation of pathogenic protein and is a novel cancer therapy. It uses the endogenous ubiquitin‐protease system (UPS), attracting ubiquitin and covering the target protein in it, thus resulting in its complete degradation of the protein interest (POI). The potential advantages of PROTAC technology compensate for the shortcomings of traditional cancer therapy and allow them to target “undruggable” proteins, which promote its rapid development in recent years. The review focuses on the mechanisms of PROTACs, discusses application of PROTACs targeting different oncogenic proteins and analyzes the strategies for designing efficient PROTACs. Collectively, the review provides references for future application of PROTACs in cancer treatment.