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.
- Usama, S. M., Park, G. K., Nomura, S., Baek, Y., Choi, H. S., & Burgess, K. (2020). Role of Albumin in Accumulation and Persistence of Tumor-Seeking Cyanine Dyes. Bioconjugate Chemistry. 31(2), 248-259.
- Whisenant, J., & Burgess, K. (2020). Blocking Coronavirus 19 Infection via the SARS-CoV-2 Spike Protein: Initial Steps.. ACS MEDICINAL CHEMISTRY LETTERS. 11(6), 1076-1078.
- Zhao, B., & Burgess, K. (2019). TrkC-Targeted Kinase Inhibitors And PROTACs. Molecular Pharmaceutics. 16(10), 4313-4318.
- Usama, S. M., Jiang, Z., Pflug, K., Sitcheran, R., & Burgess, K. (2019). Conjugation of Dasatinib with MHI-148 Has a Significant Advantageous Effect in Viability Assays for Glioblastoma Cells. CHEMMEDCHEM. 14(17), 1575-1579.
- Thavornpradit, S., Usama, S. M., Lin, C., & Burgess, K. (2019). Protein labelling and albumin binding characteristics of the near-IR Cy7 fluorophore, QuatCy. ORGANIC & BIOMOLECULAR CHEMISTRY. 17(30), 7150-7154.
- Burgess, K. (2018). Targeted theranostics featuring near infra-red dyes. ACS Photonics. 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 Photonics. 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 Photonics. 255,
- Usama, S., & Burgess, K. (2018). Near-infrared zwitterionic dye to target TrkC expressing cancer cells. ACS Photonics. 255,
- Zhao, B., Taechalertpaisarn, J., & Burgess, K. (2018). New photoaffinity labeling module. ACS Photonics. 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.
- 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
- Association of Former Students Distinguished Achievement Awards, The conferred by Texas A&M University - (College Station, Texas, United States) - For Research 2010
- 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)
- Zhou, Hua (2014-12). Synthesis and Application of Useful Organic Building Blocks and Cyclic Tetrapeptide. (Master's Thesis)
- Khumsubdee, Sakunchai (2013-12). Synthesis and Application of New Ligands Derived from N-Heterocyclic Carbenes, Phosphines and Phosphites for Asymmetric Hydrogenations. (Doctoral Dissertation)
- Ko, Eunhwa (2012-05). Exploring Key Orientations of Small Molecules to Disrupt Protein-protein Interactions. (Doctoral Dissertation)