La Jolla, CA, September 15, 2010 Scientists at The Scripps Research Institute have designed a new molecular test that will allow researchers to look for potential drugs targeting a human metabolic enzyme believed to stimulate the appetite and play a role in diabetes.
The new test, which the scientists call a simple assay, will allow researchers to look through hundreds of thousands of compounds for those that have potential to block the action of an enzyme known as ghrelin O-acyltransferase (GOAT). If drugs can be found that safely suppress the action of GOAT, they may help people who have clinical problems with appetite, obesity, and diabetes.
"There hasn't been a simple screen until now," says Kim D. Janda, Ph.D., a professor in the Departments of Chemistry and Immunology and Microbial Science, member of The Skaggs Institute for Chemical Biology, and director of The Worm Institute for Research and Medicine at Scripps Research.
Janda and Amanda Garner, Ph.D., a research associate in his laboratory, describe the new approachwhich may also prove useful for investigating other enzymes involved in a variety of diseasesin an advance, online Early edition of the journal Angewandte Chemie on September 15, 2010.
A Tempting Target
Even though GOAT was only discovered recently, in 2008, scientists had speculated for years that it had to exist. After all, its target (ghrelin, or the "G" in the acronym GOAT) had been known for more than a decade.
Ghrelin, a small peptide hormone that is mainly produced in the stomach, signals hunger, typically before meals. Ghrelin has been associated with Prader-Willi syndrome a common genetic cause of childhood obesity in which patients have exceptionally high ghrelin levels.
The biology of ghrelin is quite intricate. For ghrelin to impact the body's metabolism, it must move from the stomach to the brain, where it acts on neurons. GOAT acts as a "passpor
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Scripps Research Institute