Our research aims to develop innovative synthetic methodologies and therapeutic approaches, and apply them to solving pressing problems of biological and medical importance. New synthetic methodologies and strategies (e.g. non-traditional disconnections and C-H functionalization) have great impacts on the discovery of transformational medicines by enabling the rapid and efficient synthesis of novel, diverse, and complex biologically active molecules. New therapeutic approaches (e.g. targeted covalent inhibition and targeted protein degradation) provide new opportunities to address traditionally "undruggable" disease targets.
We anticipate that the combination of the efforts in the development of novel synthetic methodologies and therapeutic approaches will advance drug discovery in diseases of unmet need, and achieve the research goal of identifying small-molecule probes and drug candidates that specifically remove/inhibit disease-causing proteins in cells and animal models and ultimately impact human health. Representative research directions include:
1. COVID-19 drug discovery via small-molecule-induced targeted protein inhibition and degradation
2. Late-stage functionalization of drugs and peptides & its applications in drug discovery
3. Organoboron chemistry and its medical applications
Vatansever, E. C., Yang, K. S., Drelich, A. K., Kratch, K. C., Cho, C., Kempaiah, K. R., ... Liu, W. R.
(2021).Bepridil is potent against SARS-CoV-2 in vitro. Proceedings of the National Academy of Sciences of USA.