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June 2007 Issue

A library of more than 250,000 chemical compounds—acquired by P&G over the last 10 years and recently transferred to UC—will now be used by scientists trying to identify potential “drug candidates” for specific diseases.
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Compound Library Useful for Drug Discovery

Published June 2007

Drug discovery is a multi-step process, with final products often taking more than 10 years to perfect.

Finding better and faster methods for identifying promising drug candidates is the goal of many in academia and industry. In 2006, for example, UC added a rapid screening method—a high-throughput screening system—to its drug-discovery arsenal.

Now, the university and its partners have even more ammunition at their disposal.

Procter & Gamble (P&G) has provided full access and use of its chemical compound library to UC’s Genome Research Institute (GRI).

The newly acquired library—used by scientists trying to determine the right chemical structure or drug to target a specific disease—was developed by P&G over the last 10 years and contains more than 250,000 individual chemical compounds.

When used in conjunction with the high-throughput screening (HTS) system purchased last year by the Computational Medicine Center at UC and Cincinnati Children’s Hospital Medical Center, the library will become a powerful tool for enhancing UC’s drug discovery mission.

“Our drug discovery enterprise at the GRI took a major leap forward last year with the acquisition of high-throughput screening equipment,” says Jane Henney, MD, senior vice president and provost for health affairs. “The addition of the chemical compound library—along with our existing capabilities in proteomics and computer simulation—will offer investigators the critical services needed for biomedical research and drug discovery.”

The HTS system—developed by Evotec Technologies and housed at the GRI—offers researchers the ability to rapidly test the effects of hundreds of thousands of chemical compounds on defined molecular drug targets, usually specific proteins that cause body processes to go wrong in disease.

Through screening, an entire chemical “library” of possible compounds is narrowed down to a manageable number of candidates with the desired effect on the target protein.

It’s at this point that biological researchers turn to medicinal chemists to determine which of the selected compounds is most likely to be useful.

The compounds are chosen on the basis of their ability to alter the function of targeted proteins. But chemists are also looking for the least toxic compound—one that demonstrates the greatest potency and selectivity with few or no side effects.

Once identified, potentially useful compounds, or “drug candidates,” are then further tested in specific disease models, licensed or sold to biotech or pharmaceutical companies for continued development.

“The addition of the library gives researchers at UC—and others in the region—access to what we consider to be the area’s most robust drug discovery program outside the pharmaceutical industry,” says Ruben Papoian, PhD, professor and director of drug discovery at the GRI. “It’s our hope that other institutions and companies can also benefit from this resource.”

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