Center offers medicinal chemistry, rapid screening of compounds
SAN ANTONIO (Sept. 4, 2012) — Taking home-grown discoveries — research findings observed in laboratories in San Antonio — and turning them into drugs to treat disease is the focus of the Center for Innovation in Drug Discovery (CIDD) being built at both The University of Texas Health Science Center at San Antonio and The University of Texas at San Antonio (UTSA).
The CIDD is designed to help develop drugs out of original discoveries made at the Health Science Center and UTSA to treat all forms of disease and infection.
“San Antonio has always been among the top Phase I centers in the country,” said CIDD Co-Director Bruce Nicholson, Ph.D., professor and chair of biochemistry in the School of Medicine at the UT Health Science Center. “But what we’ve not done very much is take homegrown discoveries and turn them into the next-generation drugs. This center is designed to facilitate that.”
Rapid sifting of compounds
Dr. Nicholson and Matthew Hart, Ph.D., the CIDD high-throughput screening director from the Health Science Center, are developing a High-Content/High-Throughput Screening Core Facility that will enable researchers to rapidly sift through thousands of potentially therapeutic compounds. This will be housed at the Joe R. and Teresa Lozano Long Campus of the Health Science Center starting in November, but the high-content imaging screens are already operational in temporary laboratories at the Texas Research Park.
Dr. Hart is an assistant professor/research in the Department of Molecular Medicine and a member of the Barshop Institute for Longevity and Aging Studies.
“In order to identify small molecules or peptides that can bind to a protein or impact a cellular process that could represent a good target for disease therapy, you need the capacity to test and compare thousands of compounds to see which one works the best,” Dr. Nicholson said.
“The high-throughput and high-content screening facility will bring this capability to the San Antonio research community. We will offer not only biochemical screens to test how well potential drugs bind to their targets, but we will also provide screens of live cells to assess compound effects on cell behavior,” he said.
UTSA’s medicinal chemistry core facility
Doug E. Frantz, Ph.D., and Stanton McHardy, Ph.D., in the UTSA Department of Chemistry are building a medicinal chemistry core facility in labs on the UTSA Main Campus. Dr. Frantz, the CIDD co-director, and Dr. McHardy, the CIDD Medicinal Chemistry Core director, have almost 20 years of experience between them with Merck and Pfizer.
“Several top-tier universities have established centers dedicated to the discovery and development of new drugs that will treat devastating human diseases,” said Dr. Frantz, whose vision was a driving force in the center’s formation. “The most successful of these enterprises have included faculty and research staff members who bring pharmaceutical industry experience to the table. Both Dr. McHardy and I have worked on U.S. Food & Drug Administration-approved drugs during our professional careers and we believe these experiences will greatly benefit the CIDD here in San Antonio.”
Home-grown discoveries to next-generation drugs
Taking home-grown discoveries and turning them into the next-generation drugs is particularly applicable in the case of cancer research, where for many years most of the new drugs tested at the Cancer Therapy & Research Center did not originate from the Health Science Center.
Phase I cancer studies are conducted to demonstrate a novel agent’s safety in patients whose tumors are not responding to existing therapies. Phase II and further studies define optimum use of the medications.
Protein targets, cellular processes and prospective therapies
The earliest phases of pre-clinical drug discovery can take many forms. Structural biology studies at the Health Science Center have identified many protein targets for therapy in Alzheimer’s disease, Parkinson’s disease, diabetes, cancer and other disorders, and teams are in the process of obtaining high-resolution structures of these targets. This can be very effective in guiding the design of new drugs.
In other cases, scientists in many departments at the Health Science Center and UTSA have identified specific cellular processes central to the development of a disease that present ideal targets for therapy and in some cases have identified compounds or novel plant extracts that can affect them.
“The pre-clinical advancement of new, small-molecule, drug-like candidates requires a multidisciplinary approach and a diverse platform of research support,” Dr. McHardy said. “The overall strategy for the CIDD at UTSA and the Health Science Center is to pull the successful strategies used in the pharmaceutical and biotechnology sectors and provide them to researchers to help advance small-molecule therapeutics for truly novel pharmacological targets and the treatment of numerous diseases.”
Education is another key component of the center. Currently, UTSA undergraduate and graduate students in Dr. Frantz’s laboratory are conducting research on breast cancer, prostate cancer and regenerative medicine involving stem cell differentiation, and addressing diabetes and neurodegenerative diseases such as Alzheimer’s and Parkinson’s diseases. In addition, many graduate students at the Health Science Center are involved in designing therapeutic strategies to combat these same diseases. New courses in this emerging area of academic biomedical research are being developed and could lay the groundwork for a future graduate training program between these institutions.
The new center is expected to help with recruitment of outstanding faculty and graduate students to San Antonio in the field of medicinal chemistry and drug discovery. “Fruitful interactions are also anticipated between the CIDD and the UT Health Science Center’s Institute for Integration of Medicine & Science (IIMS),” said IIMS Director Robert Clark, M.D. “Accelerating the pathway of drug discovery and development from the laboratory bench to initial testing in patients is one of our key objectives, and we are very enthusiastic about the impact that the CIDD will have in this area.”
“Texas is seeing burgeoning development in biotech and drug discovery, and this new initiative will allow our students to have research opportunities that could eventually have global impacts on therapeutic treatments for patients,” Dr. Frantz said. “I think this center will be a huge attraction and recruiting tool for us to show outstanding chemists why UTSA, working alongside the UT Health Science Center, is on a phenomenal trajectory to reach Tier One status.”
State and private funding of $3.5 million is launching the CIDD. Support from the Texas Legislature is enabling renovation of existing research space, and the Legislature also provided funds through the San Antonio Life Sciences Institute. A generous private gift soon will be announced by UTSA.
The University of Texas Health Science Center at San Antonio, one of the country’s leading health sciences universities, ranks in the top 3 percent of all institutions worldwide receiving federal funding. Research and other sponsored program activity totaled $231 million in fiscal year 2011. The university’s schools of medicine, nursing, dentistry, health professions and graduate biomedical sciences have produced approximately 28,000 graduates. The $736 million operating budget supports eight campuses in San Antonio, Laredo, Harlingen and Edinburg. For more information on the many ways “We make lives better®,” visit www.uthscsa.edu.