Swanlund Professor of Chemistry
University of Illinois at Urbana-Champaign
Seeking new strategies to prevent resistance to anti-estrogen therapies and extend the lives of breast cancer patients.
Laboratory studies are focused on the development of a new class of estrogen receptor inhibitors to block ER-dependent cell growth and tissue invasion.
These efforts can have a tremendous impact on preventing breast cancer deaths by developing powerful anti-estrogens that will stop the growth of recurrent ER-positive breast cancers.
Over 30 percent of estrogen receptor (ER)-positive breast cancers that have metastasized (spread outside the breast) are driven by mutations that induce continual ER activity. This unregulation of ER activity increases resistance to aromatase inhibitors and anti-estrogens, which are commonly used to treat ER+ breast cancers. Hence, new approaches to block the growth promoting activity of estrogen are urgently needed.
Dr. John Katzenellenbogen and colleagues will investigate a new class of ER inhibitors that fully block ER activity in breast cancer cells without eliminating the ER protein. This year, the team will continue to synthesize and optimize new compounds and then evaluate their ability to block ER-dependent cell growth and invasion, as well as their ability to break down the ER protein. The team has identified some compounds that show good activity, and they are pursuing new ideas to make them even more potent and effective.
These studies may result in new ER binding compounds that will be effective against recurrent metastatic breast cancers that are resistant to current endocrine therapy agents.
Dr. John Katzenellenbogen, Swanlund Professor of Chemistry, directs a research program at the University of Illinois at Urbana-Champaign that spans chemistry, biology, and medical applications with a particular focus on the action of estrogens in breast cancer. He is recognized internationally as a pioneer in the development of novel diagnostic and therapeutic agents for the management of hormone-regulated cancers, including the PET imaging agents FES for estrogen receptors in breast cancers and FDHT for androgen receptor in prostate cancers, both of which are widely used in the clinical development of novel anti-hormonal agents. Through his extensive work elucidating the molecular details of estrogen action in various target tissues, he has designed novel estrogens that are being actively used to elucidate estrogen actions by numerous collaborators throughout the world.
Dr. John Katzenellenbogen has been honored as a Fellow of the American Academy of Arts and Sciences on whose National Council he served for many years, he is the recipient of the Paul Aebersold Award from the Society of Nuclear Medicine, the E. B. Hershberg Award for Important Discoveries in Medicinal Chemistry, the Esselen Award for Chemistry in the Public Service, and Portoghese Medicinal Chemistry Lectureship Award from the American Chemical Society, The Royal Society of Chemistry Centenary Award, the Leading Edge Award from the Society of Toxicology, and with Dr. Benita Katzenellenbogen the Fred Conrad Koch Lifetime Achievement Award from the Endocrine Society. He has trained more than 100 doctoral students and postdoctoral fellows, and he has published more than 500 articles.