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Week of December 10, 2012

CDNM announces first grants for drug discovery research

The Center for the Discovery of New Medicines awarded its first round of grants. Eight projects across U-M will be funded.

The support allows researchers to move promising potential drugs to the next phase of development; projects will investigate new therapeutics for the treatment of cancer, of antibiotic-resistant bacteria involved in food poisoning, amphetamine addiction and other diseases.

Awards up to $50,000 support access to U-M drug discovery cores such as high-throughput screening, pharmacokinetics and medicinal chemistry cores. As the pharmaceutical industry decreases investment in early drug discovery research, more academic groups have started to identify compounds that could become drugs and to test and refine those compounds. The CDNM pilot grants provide a jump-start to these non-traditional projects to speed their progress toward commercialization and ultimately clinical use.

“We had a number of interesting proposals that reflected the diversity and breadth of drug-related research at the university,” said Rick Neubig, CDNM director. “Our hope is that we will continue to fund these projects as they move forward through the process as well as add more to U-M’s drug-discovery pipeline in the next round of funding.”

Funded projects include:

• “CNS-permeant tamoxifen derivatives for the treatment of amphetamine abuse”

Margaret Gnegy, professor of pharmacology, Medical School

In collaboration with Hollis Showalter in the Vahlteich Medicinal Chemistry Core, Gnegy will synthesize new derivatives of tamoxifen, a drug used to treat breast cancer what they found to be active against amphetamine abuse. The work also uses U-M’s pharmacokinetic lab, which is housed in the Department of Pharmacy at the Medical School and directed by Duxin Sun, associate professor in the pharmaceutical sciences department.

• “Bacterial virulence traits as targets for drug development”

Victor DiRita, professor of microbiology and immunology, Medical School

DiRita will conduct a high-throughput screen in the Center for Chemical Genomics at the Life Sciences Institute in order to identify potential drugs for the treatment of food-borne illness caused by Campylobacter jejuni, a bacteria that lives in the intestines of chickens and can cause gastroenteritis and diarrhea in humans.

The Comprehensive Cancer Center contributed support for two grant proposals to receive CDNM funding:

• “Identifying HIF2α specific transcriptional regulatory mechanisms”

Yatrik Shah, assistant professor of molecular and integrative physiology

Shah defined a pathway by which oxygen deprivation accelerates cancer tumor growth by rendering the tumor more resistant to treatment. He will conduct high-throughput screens in the Center for Chemical Genomics to identify genes that control that pathway to identify ways to block cancer growth and progression.

• “Discovery of Small-Molecule Inhibitors of the EZH2-EED Protein-Protein Interaction by High Throughput Screening”

Shaomeng Wang, professor of internal medicine

Conduct high-throughput screens in the Center for Chemical Genomics to identify potential new drugs that control aberrant gene expression in lymphoma and breast and prostate cancer. This type of drug, which targets a protein-protein interaction, has been very challenging, and the area typically is avoided by pharmaceutical companies. Success would provide a new way to block tumor growth in breast and other cancers.

For the full list of funded proposals, go to cdnm.lsi.umich.edu/grantsannounced.

The next round of grants will be awarded in the spring. For application information, go to cdnm.lsi.umich.edu.

The Center for the Discovery of New Medicines is the central hub for drug research and development at U-M.

Partners include the College of Pharmacy, Life Sciences Institute, Medical School Office of Research, Comprehensive Cancer Center, Department of Internal Medicine, Department of Pathology, The Endowment for the Basic Sciences and the Michigan Institute for Clinical and Health Research.

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