This talk highlights the development and application of chemical probes—small molecules that selectively inhibit or modulate enzyme activity—to investigate the functions of human diphtheria toxin-like ADP-ribosyl transferase enzymes (ARTD) and validate these enzymes as drug targets. Moreover, ongoing research focuses on expanding structure-activity relationship (SAR) studies to other mono-ADP-ribosyl transferases (mARTDs).

This research utilizes high-throughput crystallization trials. Advanced imaging of these trials is supported by Formulatrix Rock Imagers (RI2 and RI54). Whereas, the Integrated Crystal-Data-Traking Enhancing Biochemistry Education And Research (ICEBEAR) system streamlines the process of data management and analysis. Together, these tools are playing a vital role in accelerating drug discovery and advancing structural biology research.