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.