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.
- Arancillo, M., Taechalertpaisarn, J., Liang, X., & Burgess, K. (2021). Piptides: New, Easily Accessible Chemotypes For Interactions With Biomolecules. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION. 60(12), 6653-6659.
- Usama, S. M., & Burgess, K. (2021). Hows and Whys of Tumor-Seeking Dyes.. Accounts of Chemical Research. 54(9), 2121-2131.
- Lin, C., Jiang, Z., Gao, Z., Arancillo, M., & Burgess, K. (2021). Small molecules targeting the NEDD8·NAE protein–protein interaction. Chemical Science. 12(4), 1535-1543.
- Tian, C., & Burgess, K. (2020). PROTAC Compatibilities, Degrading Cell‐Surface Receptors, and the Sticky Problem of Finding a Molecular Glue. ChemMedChem. 16(2), 316-318.
- Mi, T., & Burgess, K. (2020). Striking Similarities between CDRs in Some mAbs That Neutralize COVID-19.. ACS Medicinal Chemistry Letters. 11(9), 1663-1666.
- Burgess, K. (2018). Targeted theranostics featuring near infra-red dyes. ACS National Meeting Book of Abstracts. 256,
- 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?. ACS National Meeting Book of Abstracts. 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. ACS National Meeting Book of Abstracts. 255,
- Usama, S., & Burgess, K. (2018). Near-infrared zwitterionic dye to target TrkC expressing cancer cells. ACS National Meeting Book of Abstracts. 255,
- Zhao, B., Taechalertpaisarn, J., & Burgess, K. (2018). New photoaffinity labeling module. ACS National Meeting Book of Abstracts. 255,
- Saragovi, H., & Burgess, K. (2005). ?-turn peptidomimetic cyclic compounds.
- Burgess, K. (2002). Ligands for chiral catalysis.
- Burgess, K., & Gibbs, R. (2002). Through bond energy transfer in fluorescent dyes for labelling biological molecules.
- 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
- Humboldt Research Award conferred by Alexander von Humboldt Foundation - (Bonn, Germany) 2015
- Fellow conferred by Royal Society of Chemistry - (London, United Kingdom) 2013
- Pedler Award conferred by Royal Society of Chemistry - (London, United Kingdom) 2013
- 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)
- Xin, Dongyue (2016-05). Design and Synthesis of Small Molecules to Target Protein-Protein Interactions. (Doctoral Dissertation)