Patients with metastatic breast cancer—when the tumor has spread to other organs in the body—face a terminal prognosis and toxic treatments. There is an urgent need for new ways to treat drug metastatic and resistant stages of the disease. Sarat Chandarlapaty, MD, PhD (Damon Runyon Clinical Investigator ’12-’17), and colleagues, have developed a novel class of drugs that may help these patients by potentially stopping or even destroying breast cancer tumors. The drugs can attach to the estrogen receptors (ER) in cancer cells and then hijack the cell's protein-disposal machinery to degrade the receptor. The new compounds also block the hormone estrogen from binding to its receptor. As a result, breast cancer cells in the laboratory stopped growing and multiplying. 

"Over the years, the roles of the ER in mediating tumor growth in breast cancer has gained importance, but current therapies targeting ER lack potency or work for a short time only. This new class of drugs eliminates the receptor through degradation, perhaps preventing relapse," says Sarat. The researchers plan to next test these compounds in animal models of cancer, with the hope of eventually moving them to clinical trials in humans. The research was published in the American Chemical Society ACS Medicinal Chemistry Letters.