Rui Xiong

The Xiong lab is focused on the structure-based design of bioactive molecules to modulate disease-causing proteins or genes. We use modern molecular biology tools to develop biochemical, biophysical, and cellular assays to screen and optimize molecules for various therapeutic targets. Our projects also heavily utilize X-ray crystallography and computational modeling to guide molecule design. Two novel molecules developed from this pipeline successfully entered human clinical trials for treating advanced breast cancer (NCT03201913: Xiong R., et al., J Med Chem. 2016, 59, 219-237; NCT03455270: Xiong R., et al., J Med Chem, 2017, 60, 1325-1342). Current research is focused on the newly NIH RO1-funded project to develop potent SARS-COV-2 PLpro inhibitors.

We are also interested in developing novel technologies to selectively activate therapeutically relevant proteins. Traditional drug discovery research has been focused on inhibiting disease-driving proteins, while chemical tools for activating disease-causing proteins are lacking. We are interested in developing tools to study and mimic how nature selectively activates gene transcription.

Areas of Research

• Medicinal chemistry
• Bioassays
• Drug Discovery & Development
• Gene regulation