News & Events

When

Date - March 23, 2018
1:00 pm - 2:00 pm

What

Assistant Professor
Department of Medicinal Chemistry and Pharmacognosy
University of Illinois at Chicago

Abstract:

“Development of chemical probes for protein-transcription factor interactions”

The Moore Lab at UIC is interested in creating both peptidic and small molecule-based probes of protein-transcription factor interactions using the techniques of organic synthesis, medicinal chemistry, chemical biology and biochemistry. In particular, my laboratory works 1) to inhibit interactions of nuclear receptors with coactivators and 2) to inhibit the interaction of the transcription factor Nrf2 with its negative regulator, Keap1. With respect to the former project, resistance to tamoxifen occurs in 1/3 of breast cancer cases that originally responded to this targeted therapy. The estrogen receptor is still present and active in the vast majority of these cases, providing a viable target, but new ways of inactivating its function are needed. This is especially true in the case of mutant estrogen receptors, for which there are currently no selective antagonists. Our work focuses on directly inhibiting this important protein-protein interaction with “stapled” peptides. With respect to the second project, our lab is interested in inhibiting the Nrf2/Keap1 interaction with reversible, small molecule inhibitors. Given the importance of Nrf2 in cytoprotection and tissue repair, these inhibitors of the Keap1/Nrf2 interaction are of current considerable interest to the field.