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Targeted protein degradation (TPD) is under intensive focus with respect to the next-generation drugs to target currently undruggable proteins. Bivalent type degraders, known as proteolysis-targeting chimeras (PROTACs), are an attractive but challenging novel modality. As drug discovery for TPD involves time-consuming and costly processes, it is important to establish a platform for not only the identification and validation of the targets but also rapid and efficient drug discovery. Herein, two processes were proposed: (1) target validation by a ligand-induced genetic degradation system, especially the Auxin-Inducible Degron (AID) system and (2) degrader drug discovery by Rapid Protein Proteolysis Inducer Discovery System (RaPPIDSTM). Moreover, a strategy was developed for the discovery of TPD drugs against novel target proteins.

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