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The pathway of protein post-translational modification (PTM) play a crucial role in variouspathophysiological conditions, indicating the promising target for personalized medicine.The substrates of PTM regulative enzymes and their specific inhibitors including HDAC,HMT, kinase and E3 ligase are well demonstrated as effective anti-cancer drugs, while howto comprehensively screen the biomarker and targets of those enzymes and correspondinginhibitors remains great challenges.