A team at UTSA-UT Health San Antonio is studying compounds aimed at treating brain tumors. UTSA Today | UTSA

Stanton Mchardy

UTSA chemists, including Stanton MchardyA professor in the Department of Chemistry at UTSA ., has developed molecules that mimic estrogenic activity at ER-beta without the known side effects associated with increased estrogen, such as breast tenderness and vaginal bleeding in women and fatigue and sweating in men. I am working on generating.

“In my lab, we design, synthesize and optimize small-molecule inhibitors of ER-beta,” McHardy said. “Our ultimate goal is to identify structurally novel ER-beta-hi agonists, estrogenic-like molecules that can be developed clinically.”

McHardy’s involvement in the project is personal. His older sister died of her GBM tumor, which was inoperable for which there was no effective treatment. He says the project has become a highly efficient and productive collaboration between his lab and his research partners.

McHardy is Director of the Center for Innovative Drug Discovery (CIDD), a joint initiative of UTSA and UT Health San Antonio, funded by the Cancer Prevention Institute of Texas (CPRIT). A grant from CPRIT helped provide the team with preliminary data generation support that strengthened her NCI-funded proposal.

CIDD consists of the High Throughput In Vitro Screening (HTSF) and Computer Aided Drug Design (CADD) facilities at UT Health San Antonio, as well as the Medicinal Chemistry Core Facility (MCCF) and the Pre-UTSA Clinical Pharmacology Core Facility (PCPC). The Center’s mission is to provide diverse core facilities and expertise to facilitate the translation of fundamental scientific discoveries into specific preclinical drug candidates that can later be developed into clinical treatments.

Karinel Nieves-Merced When Michael Tidwell, a CIDD Fellow, and a UTSA staff chemist contributed to the research programme. Nieves-Merced assisted in the early compound design stages of the program, and Tidwell synthesized the compound and characterized its structure.

“This research proposal is based on strong preliminary data showing that ER-beta exerts a tumor suppressor function in glioblastoma,” he said. Ratna K. Vadramdi, Professor of Obstetrics and Gynecology at UT Health San Antonio. “This proposal will lead to the development of new ER-beta drugs that promote tumor suppression and new therapeutic modalities to treat GBM.”

Scientists are conducting iterations of ER-beta agonists to develop new clinical strategies and bring hope to patients and families affected by GBM. The goal is to complete validation using preclinical models and test the molecule in clinical trials in two to three years.

“This is a great example of drug discovery that is making a real impact on cancer treatment here at UTSA,” he said. Audrey Lamb, Professor and Chair of the Department of Chemistry, UTSA. “I am very excited about the research that Dr. McHurdy and his team are conducting and it has clear potential to provide therapeutic strategies in the near future.”