KU News Release
June 23, 2011
Contact: Brendan Lynch, University Relations, 785-864-8855
KU researchers win $1.5 million to press forward with therapies for drug addiction
LAWRENCE — Drug addiction destroys lives, tears apart families and harms society. The National Survey on Drug Use and Health reported that 8 percent of the population aged 12 or older were current users of illicit drugs in 2008.
Now, medicinal chemistry researchers at the University of Kansas have earned a five-year, $1.5 million grant from the National Institutes of Health to build new compounds that someday may help people struggling with drugs such as cocaine and heroin.
“If we’re really lucky, some of those compounds may advance into a drug-discovery project,” said Jeff Aubé, professor of medicinal chemistry and principal investigator of the grant. “What we’re trying to do now is determine the relationship between the structure of a molecule and its biological activity.”
Aubé leads teams at the Specialized Chemistry Center and Center of Excellence in Chemical Methodologies and Library Development at KU that together have developed and improved five classes of molecules, or chemical compounds, that show promise for addiction treatment. The molecules first were singled out from a group of 300,000 molecules tested by the Sanford–Burnham Research Medical Institute, a member of the NIH-supported Molecular Libraries Probe Production Centers Network. KU’s Specialized Chemistry Center is also a part of the same network.
“What this new grant is for is to explore those compounds and derivatives of those compounds at further depth,” Aubé said. “It will allow us to take these a step beyond — to really allow us to understand what these compounds are doing in their biological setting.”
The molecules are designed to interact with kappa opioid receptors, located within neurons in the human spine, which play a role in drug dependency.
“New molecules that act at that receptor are of interest because that receptor is implicated in a lot of things besides the reduction of pain,” said Aubé. “It’s implicated in addiction behavior because it helps to mediate levels of dopamine that are present in the brain.”
The medicinal chemistry researchers at KU will work with pharmacologist Laura Bohn, research associate professor at the Scripps Research Institute in Jupiter, Fla. Bohn will test molecules developed at KU against opioid receptors isolated in test tubes and mice to gauge their potential.
“You start off with a molecule that has a particular chemical structure and you measure the biological response,” said Aubé. “Then you change the structure a little bit and you see how that change affects the biology.”
The grant will make possible two new research positions at the Structural Biology Center on KU’s west campus and fund graduate student research. Down the road, the researchers at KU and Scripps even may be able to patent chemicals that show likely potential as drug therapies for addiction.
“This grant is strictly for the basic medicinal chemistry and pharmacology,” said Aubé. “But if we have exciting compounds, KU and Scripps will certainly patent those compounds and will seek to develop them so that a drug company could actually bring them all the way through to the clinic. But we’re a long way from that point.”
Aube emphasized the collaborative nature of the research at KU, citing important contributions by Kevin Frankowski, research associate; Frank Schoenen, courtesy associate professor of medicinal chemistry; Tom Prisinzano, associate professor of medicinal chemistry; and staff scientists Stephen Slauson, Partha Ghosh, David Whipple and Kelin Li.
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