Stanton McHardy, UTSA associate professor of chemistry and director for the Center of Innovative Drug Discovery (CIDD), is collaborating with UT Health Science Center professor of molecular medicine Rong Li on a breast cancer drug discovery research partnership. The partnership recently received $1.9 M from the Cancer Prevention & Research Institute of Texas (CPRIT).

Collaboration between the institutions started last year. Researchers will use the grant money to identify small molecules as drug candidates for triple negative breast cancer – a rare form of cancer with a high mortality rate. Triple negative breast cancer is associated with Estrogen Receptor beta. Dr. Li and Dr. McHardy refer to ER beta as the “Cinderella Sister” – it is similar to ER alpha, but instead of promoting tumor growth, ER beta inhibits it. “If there is a way to modulate ER Beta’s activity, then it might provide an avenue for treating triple negative breast cancer,” says McHardy.

UTSA and the Health Science Center implemented a pilot proposal to target small molecules that could modulate ER beta pathways. “The proposal got funded, and we are designing small molecules that inhibit EY2, which can promote ER beta activity,” says McHardy. “We have a lot of data showing that these molecules will kill cancer cell lines.”

The Pilot program’s encouraging data played a key role in receiving the CPRIT grant. “The idea is to take novel drug discovery targets and to get them ready for pre-clinical testing in a short time period,” says McHardy. “It is an aggressive proposal. Normally, it takes three to five years to go from early discovery to more involved pre-clinical evaluation of small molecules; we are targeting a three-year time frame.”

Breast cancer drug research will help grow the CIDD, the drug discovery efforts and the cancer portfolio at UTSA. “As we develop new classes of molecules, we will be submitting patent applications and literature reports,” says McHardy. “If we find something that is really good and eventually get a licensing opportunity, then that can bring back revenue to UTSA.”

Experienced chemists like McHardy will be coming up with synthetic routes for the targeted small molecules. Students working alongside the research are also going to receive real drug discovery experience. “I will sit with the students, and we will design new molecules that we think will be active for the ER beta function we want to impact,” says McHardy. “The students’ job will be to run the chemistry and to figure out the best synthetic route to make the compound.”

According to McHardy, whose background is in the pharmaceutical industry, the CIDD has been an attraction to students because of the top-notch equipment and research experiences it makes available for UTSA students. “We joke, but only half joke, when we say that these labs are nicer than what we had at Pfizer,” says McHardy.

McHardy emphasizes the interdisciplinary nature of the research and traces the program’s success to the collaboration efforts between molecular biology, chemistry, drug metabolism and clinical oncology. “We have all of those components working together as a team,” says McHardy.

After losing his father and sister to cancer, McHardy was motivated to focus his research on finding effective and innovative tumor treatments. Initiatives like UTSA’s and the Health Science Center’s collaborative research offer hope for the development of successful next generation breast cancer drugs.

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