Jung-Mo Ahn is an Associate Professor of Chemistry, focusing on bio-organic and medicinal chemistry. Through his research he is seeking to understand the chemistry and biology of peptides and proteins, and to develop new approaches for manipulating these properties with purposefully designed small organic molecules. His projects include:
Development of peptidomimetics for the treatment of Diabetes Mellitus
Development of therapeutic agents for biodefense against bacterial infection
Rational design of small molecules for mimicking protein secondary structures to modulate protein-protein interactions involved in cancer
Development of metabolically stable peptides as molecular imaging agents for non-invasive assessment of pancreatic beta-cells
The majority of human breast cancer is estrogen receptor alpha (ER) positive. While anti-estrogens/aromatase inhibitors are initially effective, resistance to these drugs commonly develops. Therapy-resistant tumors often retain ER signaling, via interaction with critical oncogenic coregulator proteins. To address these mechanisms of resistance, we have developed a novel ER coregulator binding modulator, ERX-11. ERX-11 interacts directly with ER and blocks the interaction between a subset of coregulators with both native and mutant forms of ER. ERX-11 effectively blocks ER-mediated oncogenic signaling and has potent anti-proliferative activity against therapy-sensitive and therapy-resistant human breast cancer cells. ERX-11 is orally bioavailable, with no overt signs of toxicity and potent activity in both murine xenograft and patient-derived breast tumor explant models. This first-in-class agent, with its novel mechanism of action of disrupting critical protein-protein interactions, overcomes the limitations of current therapies and may be clinically translatable for patients with therapy-sensitive and therapy-resistant breast cancers.