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Finding of long-sought drug target structure may expedite drug discovery
Date:3/15/2011

Researchers have solved the three-dimensional structure of a key biological receptor. The finding has the potential to speed drug discovery in many areas, from arthritis to respiratory disorders to wound healing, because it enables chemists to better examine and design molecules for use in experimental drugs.

The researchers are from the National Institutes of Health, collaborating with labs at The Scripps Research Institute and the University of California, San Diego. The finding is published in the March 10 edition of Science Express.

"This is an important step forward it was impossible until recently to know how this type of receptor is switched on by chemical signals like a tiny machine," said Dr. Kenneth A. Jacobson, chief of the Laboratory of Bioorganic Chemistry in NIH's National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) and an author on the paper. "The architecture of the activated receptor allows us to think in more detailed terms about the other half of the drug interaction. We hope that we're on the verge of a revolution that will expedite the process of crafting new drugs to treat disease."

With this finding, scientists in Jacobson's lab, including co-author Dr. Zhan-Guo Gao, will next work on testing this drug-engineering approach with similar molecules they have newly synthesized.

Jacobson and Gao are part of the NIDDK's intramural program, which enables basic scientists and clinicians of diverse skills and expertise to collaborate on solutions to some of the most difficult issues of human health. Several compounds from Jacobson's lab are currently in clinical trials as potential treatments for conditions including chronic hepatitis C, psoriasis and rheumatoid arthritis.

"Discoveries like this, with the potential to lead to future treatments in a wide variety of areas, are why NIH funds basic science," said NIDDK Director Dr. Griffin P. Rodgers. "By understanding the
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Contact: Amy Reiter
NIDDKMedia@mail.nih.gov
301-496-3583
NIH/National Institute of Diabetes and Digestive and Kidney Diseases
Source:Eurekalert  

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