Insights into opioid receptors help tailor new drugs
Chemist Philip Portoghese of St. Paul, Minn., will be honored on March 28 by the world's largest scientific society for revealing precisely how drugs such as morphine interact with opioid receptors -- information that can be used to tailor-make new drugs, for example. He will receive the Alfred Burger Award in Medicinal Chemistry from the American Chemical Society at its 219th national meeting in San Francisco.
Like other biologically active compounds, opioids -- drugs derived from opium, such as morphine and heroin -- work by binding to receptors, specific protein pockets on the surfaces of cells.
"As researchers gain more insight into how molecules and receptors actually recognize each other, they can tailor-make drug molecules that are more effective or more selective," explained Portoghese, a medicinal chemist at the University of Minnesota. "And we can gain insight into how molecules bind by modifying them and their receptors in a systematic way."
For example, his team has developed genetic tools used to replace a bulky receptor building block with a smaller one, or a negatively charged receptor with a neutral one. The team analyzes whether and how much a molecule will bind to the modified receptor. "By feeding that information back into computer, we can refine our receptor models," Portoghese said.
In addition to basic research, he studies molecules as potential new drugs that could be used to treat opioid and cocaine addictions, or as painkillers with a lower risk of dependency. And Portoghese has been editor of the Journal of Medicinal Chemistry for 28 years.
Alfred Burger, the professor emeritus in chemistry at the University of Virginia for whom the award is named, characterizes Portoghese as "a chemist of so many interests that one can only guess whether he ever has time to rest."
Portoghese said his father was a pharmacist, "so I was able to make my own chemistry set even when I was a little kid. But I was also interested in art," he added. Noting that he ended up choosing the "practical" career, he said: "It's turned out that conducting research is a good outlet for creativity, too."
The Alfred Burger Award in Medicinal Chemistry is sponsored by SmithKline Beecham of King of Prussia, Pa.
A nonprofit organization with a membership of 161,000 chemists and chemical engineers, the American Chemical Society www.acs.org publishes scientific journals and databases, convenes major research conferences, and provides educational, science policy and career programs in chemistry. Its main offices are in Washington, D.C., and Columbus, Ohio.