image: GOAT activates ghrelin by acylation, attaching a fatty acid. To block this acylation and thus ghrelin signaling, we designed GO-CoA-Tat, a "bisubstrate" compound that incorporates both ghrelin and an activated fatty acid in one molecule. This allows it to tightly lock into the active site of GOAT, and the compound potently inhibits ghrelin signaling both in vitro and in mice, preventing weight gain and improving blood sugar. This image relates to an article that appeared in the Nov. 18, 2010, issue of Science Express, published by AAAS. The study, by Brad P. Barnett of The Johns Hopkins University School of Medicine in Baltimore, Md., and colleagues was titled, "Glucose and Weight Control in Mice with a Designed Ghrelin O-Acyltransferase Inhibitor." view more
Credit: Image courtesy of <i>Science/</i>AAAS