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. no-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:
- COVID-19 drug discovery via small-molecule-induced targeted protein inhibition and degradation
- Late-stage functionalization of drugs and peptides & its applications in drug discovery
- Organoboron chemistry and its medical applications
- Postdoctoral fellow, Purdue University (2013)
- Ph.D. in Medicinal Chemistry, Fudan University (2009)
- Cao, W.; Cho, C.-C. D.; Geng Z. Z.; Ma, X. R.; Allen, R.; Shaabani, N.; Vatansever, E. C.; Alugubelli, Y. R.; Ma, Y.; Ellenburg, W. H.; Yang, K. S.; Qiao, Y.; Ji, H.*; Xu, S.*; Liu, W. R.* Evaluation of SARS-CoV-2 main protease inhibitors using a novel cell-based assay. ACS Cent. Sci., 2022, 8, 192-204.
- Alugubelli, Y. R.; Geng, Z. Z.; Yang, K. S.; Shaabani, N.; Khatua, K.; Ma, X. R.; Vatansever, E. C.; Cho, C.-C.; Ma, Y.; Xiao, J.; Blankenship, L. R.; Yu, G.; Sankaran, B.; Li, P.; Allen, R.; Ji, H.*; Xu, S.*; Liu, W. R.* A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals. Eur. J. Med. Chem. 2022, 240, 114596.
- Cheng, H.; Yang, T.; Edwards, M.; Tang, S.; Xu, S.*; Yan, X*. Picomole-scale transition metal electrocatalysis screening platform for discovery of mild C–C coupling and C–H arylation through in situ anodically generated cationic Pd. J. Am. Chem. Soc. 2022,, 144, 1306-1312.
- Fu, X.; Qi, Q.; Xu, S.*; Negishi, E. Chemo-and stereoselective dearomative coupling of indoles and bielectrophilic β-imino boronic esters via imine-induced 1,2-boronate migration. Org. Lett. 2021, 23, 8984-8988.
- Qi, Q.; Yang, X.; Fu, X.; Xu, S.*; Negishi, E*. Highly enantiospecific borylation for chiral α‐amino tertiary boronic esters. Angew. Chem. Int. Ed., 2018, 57,, 15138-15142.