VAI Finding Could Lead to New Drugs for Anxiety, ...( Researchers determine molecular str...),Health

Researchers determine molecular structure of promising drug target using

new method

GRAND RAPIDS, Mich., Oct. 15 /PRNewswire/ -- Researchers in the Laboratory of Structural Sciences at Van Andel Institute (VAI) have determined how the hormone corticotrophin releasing factor (CRF) precisely binds to its receptor. This detailed structural information can help drug developers design new drugs for anxiety, depression, and related disorders.

"There are a few drugs in development to treat anxiety, depression, and other conditions by targeting the cellular receptor that CRF binds to, but there are no drugs currently on the market," said VAI Distinguished Scientific Investigator Eric Xu, Ph.D., who published his laboratory's findings in The Journal of Biological Chemistry. "There is a lot of interest in this receptor as a drug target, and we are the first to determine the structural details necessary to develop an ideal drug."

CRF is a hormone and neurotransmitter secreted by the hypothalamus area of the brain and is involved in stress response. CRF has been associated with anxiety, depression, and related disorders. The hormone's receptor is a protein on the surface of a cell or in its interior that binds to the hormone, which allows the hormone to activate changes in the cell.

Using a technique known as X-ray crystallography, VAI researchers determined the molecular structure of the part of the CRF receptor that sticks outside of the cell and binds to CRF and other proteins in the same family. This detailed structural information can help drug developers engineer a drug that more perfectly fits to the receptor, making the drug more potent. Researchers determined the structure of the receptor in three different scenarios -- one with nothing bound to the receptor, one with CRF bound to the receptor, and one that shows how the receptor binds to other proteins in the same family.

To determine the struc
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