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 develobiochemical, 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 developotent SARS-COV-2 PLpro inhibitors.