Dr. Glenn Micalizio, Department of Pharmaceutical Sciences professor and Susan & Henry Samueli Endowed Chair in Integrative Health, published a study entitled “An Estrogen Receptor β Agonist with AR Antagonist Activity from a Modern Asymmetric De Novo Steroid Synthesis” in ACS Medicinal Chemistry Letters.
The study, which was authored along with researchers from The Ohio State University and Dartmouth College, builds on previous work and describes how molecular synthesis technology was used to alter the medicinally relevant properties of a steroidal lead.
“Following up on our earlier discovery of the most potent and selective agonist of the tumor suppressor estrogen receptor beta (ERβ), we report studies that have resulted in discovery of a novel steroidal molecule that is both a potent and selective agonist of ERβ, while also possessing activity as an antagonist of the androgen receptor (AR),” Dr. Micalizio explained. “This dual activity (polypharmacology) is of potential interest for the development of a new class of prostate cancer therapeutics.”
As a continuation of this research in the future, the team aims to further study and optimize the drug-like properties of the steroidal lead, with the ultimate goal of arriving at a clinically relevant agent.
