Quantitative Chemoproteomic Profiling of Targets of Au(I) Complexes by Competitive Activity-Based Protein Profiling

Owing to the encouraging pharmacological action and acceptable toxicity profile, Au­(I) complexes have attracted growing interest in the application of disease treatment. In order to investigate their potential target proteins and related bioinformation, herein, we screened four Au­(I) complexes and explored the binding proteins utilizing a competitive activity-based protein profiling (ABPP) strategy, including identification experiments and reactivity classification experiments, which offers a simple and robust method to identify the target proteins of Au­(I) complexes. We quantified the target proteins of the four Au­(I) complexes and found that most of proteins were associated with cancer. In addition, the newly Au­(I)-binding proteins and biological gold–protein interaction pathways were exhibited. Furthermore, we estimated the correlation between target proteins of Au­(I) complexes and various cancers, which will promote the development of the gold anticancer drugs.