Speeding Drug Discovery with the Chemistry-Biology Centers Program

Advancements in genetic chemistry are making it possible to develop millions of potential cancer drugs in a matter of weeks or months, rather than years. To further this fast-forward drug screening, the National Cancer Institute recently awarded $5.5 million to create Chemistry-Biology Centers at Harvard University (co-funded by Merck and Co., West Point, Pa.); the University of Pittsburgh; Torrey Pines Institute for Molecular Studies in San Diego; and the Scripps Research Institute in La Jolla, Calif. Another $3 million has been set aside for additional new centers, to be named in 1999.

These centers will work to develop and refine robotic drug production and screening technology, which spring from the burgeoning field of combinatorial chemistry. Working with these automated methods, chemists and biologists will be able to manufacture and test potential anti-cancer drugs hundreds of times faster than with older techniques.

The discovery of scores of cancer-causing or promoting genes generated the need for this high-volume drug screening. Every newly found gene, along with the protein it produces, offers a new molecular target for an anti-cancer drug. Finding drugs -- molecules -- that are the right size and shape to fit these binding sites has traditionally been a slow, tedious search -- akin to picking through dozens of hardware bins to find just the right gear.

But with this new technology, researchers can quickly produce an array of molecules then test them for anti-cancer activity. So instead of picking through bins of gears one by one, researchers can quickly scan the whole hardware store. Finding a hit or near-miss yields a template molecule, which researchers can use to churn out hundreds of similar molecules. Then they repeat the scanning, looking for a bulls-eye. Finally, all the molecular hits and misses can be warehoused in a database, where other researchers can glean time-saving tips.

Pharmaceutical companies have rushed to develop these technologies, which increase drug-screening rates a hundredfold or more. This market-driven desire to bring more new drugs to market has already born some early rewards: Within the past two years, several companies have announced discovering potential anti-cancer and anti-HIV drugs using automated drug development and screening. However, it is still too early to tell if these new drugs will be safe and effective in people.

Bringing together top researchers in the Chemistry-Biology Centers Program will allow the National Cancer Institute to train these powerful new tools on inventing novel anti-cancer drugs. By pooling knowledge from four critical fields -- chemistry, biology, genetics, and computer science -- this interdisciplinary effort promises to proffer new cancer drugs within a few years.

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