'Click-made' biaryl-linker improving efficiency in protein labelling for the membrane target protein of a bioactive compound

摘要

We report on the design, synthesis and assessment of a novel biaryl-linked (BArL) molecular probe for the exploration of low-abundant target proteins for bioactive compounds based on the activity based protein profiling (ABPP) approach. Surprisingly, the performance of the BArL probe was better than that of the stepwise tagging approach that is considered to be the most effective method used in ABPP study. Activity-based protein profiling (ABPP) has become a powerful strategy for understanding biological processes in living cells and organisms. Because most target proteins for bioactive natural products are unknown, the prospect of using ABPP with a bioactive natural product to induce a physiologically intriguing phenomenon would launch a new field of chemical biology.