Medicinal Chemistry, Director
Our medicinal chemistry efforts are project based with a faculty generated lead compound. We can support 3-5 hit to probe/lead projects concurrently. The typical timeline from completion of a screen to completion of leads is 1-2 years. Projects are prioritized primarily based on quality of hits and project funding. To date our most successful project has been the development of inhibitors of Mer kinase for the treatment of leukemia and immunosuppressive tumors. A significant portion of this work was funded through a research contract as a member of NCI’s Chemical Biology Consortium (CBC). In addition, we were funded through the CBC to conduct structure activity relationship (SAR) studies to support lead development of inhibitors of IDH1 to treat glioblastoma. We have contributed to numerous drug discovery efforts with UNC faculty and external investigators.
- Zhou, Y.; Mukherjee, S.; Huang, D.; Chakraborty, M.; Gu, C.; Zong, G.; Stashko, M. A.; Pearce, K. H.; Shears, S. B.; Chakraborty, A., Wang, H.; Wang, X. Development of Novel IP6K Inhibitors for the Treatment of Obesity and Obesity-Induced Metabolic Dysfunctions. J Med Chem 2022, 65 (9), 6869. 10.1021/acs.jmedchem.2c00220.
- Yan, D.; Huelse, J. M.; Kireev, D.; Tan, Z.; Chen, L.; Goyal, S.; Wang, X.; Frye, S. V.; Behera, M.; Schneider, F.; Ramalingam, S. S.; Owonikoko, T.; Earp, H. S.; DeRyckere, D.; Graham, D. K., MERTK activation drives osimertinib resistance in EGFR-mutant non-small cell lung cancer. J Clin Invest 2022, 132 (15), e150517.