We use novel strategies Exploring Key Orientations (EKO) that feature datamining to compare simulated preferred conformers of chemotypes we design with key features at protein-protein interfaces. Many chemotype candidates can be screened against one PPI, or one chemotype can be screened against all the PPI interfaces in the PDB. Virtual hit chemotypes are prepared in my lab, then tested against protein-protein interactions of biomedicinal interest using an array of biophysical and cellular assays.
We also design small molecules to target cell surface receptors that are selectively overexpressed in cancer cells. Much or our work has been focused on the TrkC receptor that is particularly important to metastatic breast cancer and melanoma. Going forwards we are interested in expanding the targets to include cell surface receptors that are overexpressed when cancer cells undergo aberrant epithelial to mesenchymal transitions (EMT) to produce circulating tumor cells and cancer stem cells. Much of this work involves design and synthesis of the small molecules for this targeting.
Academic Articles266
- Arancillo, M., Taechalertpaisarn, J., Liang, X., & Burgess, K. (2021). Piptides: New, Easily Accessible Chemotypes For Interactions With Biomolecules. 60(12), 6653-6659.
- Tian, C., & Burgess, K. (2021). Flavylium‐ and Silylrhodapolymethines In Excitation Multiplexing. 5(8), 702-704.
- Usama, S. M., Zhao, B., & Burgess, K. (2021). Fluorescent kinase inhibitors as probes in cancer. 50(17), 9794-9816.
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- Guo, M., Wang, G., Zhao, Y., Li, H., Tang, K., Zhao, Y., & Burgess, K. (2021). Preparation of Nano-ZrO2 powder via a microwave-assisted hydrothermal method. 47(9), 12425-12432.
Conference Papers91
- Taechalertpaisarn, J., Araneillo, M. N., Lin, C., Lyu, R., Jiang, Z., Perez, L., Loerger, T., & Burgess, K. (2018). How relevant is secondary structure mimicry in design of small molecules to disrupt protein-protein interfaces?. 255,
- Wanichacheva, N., Tachapermpon, Y., Praikaew, P., Thavornpradit, S., Charoenpanich, A., Sirirak, J., & Burgess, K. (2018). Near-infrared aza-BODIPY fluorescence probes for selective Cu2+detection and their potential in living cell imaging. 255,
- Usama, S., & Burgess, K. (2018). Near-infrared zwitterionic dye to target TrkC expressing cancer cells. 255,
Patents4
- Burgess, K., & Gibbs, R. (2002). Through bond energy transfer in fluorescent dyes for labelling biological molecules.
Principal Investigator5
- Evaluation of Trk Probes in Models for Dry Eye Disease awarded by DHHS-NIH-National Eye Institute 2019 - 2022
- CDS&E: Cyclic Tetrapeptide Probes for Protein Binding awarded by National Science Foundation 2016 - 2020
- Theranostics Targeting Metastatic Breast Cancer awarded by DOD-Army-Medical Research and Materiel Command 2015 - 2019
- CHEM227 Hnr-organic Chemistry I Instructor
- CHEM228 Hnr-organic Chemistry Ii Instructor
- CHEM231 Tech Of Organic Chem Instructor
- CHEM491 Hnr-research Instructor
- CHEM491 Research Instructor
- Zhao, Bosheng (2020-04). Small Molecules for Active Targeting and Development of PROTACs. (Doctoral Dissertation)
- Zhao, Bosheng (2020-05). Small Molecules for Active Targeting and Development of PROTACs. (Doctoral Dissertation)
- Jiang, Zhengyang (2019-08). Development of Novel Theranostic Small Molecules for Cancer Treatment. (Doctoral Dissertation)
- Usama, Syed Muhammad (2019-08). Developing Targeted Theranostic Agents for Tumors. (Doctoral Dissertation)
- Taechalertpaisarn, Jaru (2018-05). Design, Optimization and Syntheses of Small Molecules to Disrupt Protein-Protein Interactions. (Doctoral Dissertation)