Research Interests
Molecular Glue and Heterobifunctional Transcription Factors Degraders in Inflammation and Cancer
Research Description
We explore and develop molecular glue and heterobifunctional small-molecule degraders of transcription factors in inflammation, cancer, and autoimmune diseases. I am looking for students interested in using cryo-EM, X-ray crystallography, and structure-based computational methods to explore the mechanism of action of these compounds and to guide the design of new and improved molecular degraders. Students will also have the opportunity to screen large libraries of small molecules for covalent and non-covalent molecular glue degraders using biochemical and cell biological assays.
Additional Campus Affiliations
Phil and Ann Sharp Scholar, Biochemistry
Professor, Biochemistry
Affiliate, Chemistry
Affiliate, Carl R. Woese Institute for Genomic Biology
Recent Publications
Landgraf, A. D., Brenner, R., Ghozayel, M. K., Bum-Erdene, K., Gonzalez-Gutierrez, G., & Meroueh, S. O. (2025). Small-Molecule KRAS Inhibitors by Tyrosine Covalent Bond Formation. ChemMedChem, 20(12), Article e202400624. https://doi.org/10.1002/cmdc.202400624
Yeh, I. J., Bum-Erdene, K., Ghozayel, M. K., Gonzalez-Gutierrez, G., & Meroueh, S. O. (2025). Small-Molecule Covalent Stabilization and Inhibition of the TEAD·YAP1 Transcription Factor in Cancer Cells. ACS chemical biology, 20(9), 2142-2158. https://doi.org/10.1021/acschembio.5c00283
Brenner, R. J., Landgraf, A. D., Bum-Erdene, K., Gonzalez-Gutierrez, G., & Meroueh, S. O. (2023). Crystal Packing Reveals a Potential Autoinhibited KRAS Dimer Interface and a Strategy for Small-Molecule Inhibition of RAS Signaling. Biochemistry, 62(22), 3206-3213. https://doi.org/10.1021/acs.biochem.3c00378
Bum-Erdene, K., Ghozayel, M. K., Zhang, M. J., Gonzalez-Gutierrez, G., & Meroueh, S. O. (2023). Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction. RSC Medicinal Chemistry, 14(9), 1803-1816. https://doi.org/10.1039/d3md00264k
Bum-Erdene, K., Yeh, I. J., Gonzalez-Gutierrez, G., Ghozayel, M. K., Pollok, K., & Meroueh, S. O. (2023). Small-Molecule Cyanamide Pan-TEAD·YAP1 Covalent Antagonists. Journal of Medicinal Chemistry, 66(1), 266-284. https://doi.org/10.1021/acs.jmedchem.2c01189