Methods for synthesis and uses of inhibitors of Ghrelin O-acyltransferase inhibitors as potential therapeutic agents for obesity and diabetes

摘要

The patent claims inhibitors of ghrelin-O-acyltransferase enzyme. These inhibitors were designed as bisubstrate analogs of the enzymatic reaction and were coupled with one of the peptides able to cross cell membranes, the 11-mer Tat peptide. The compound GO-CoA-Tat was studied in vitro and in vivo; after intra-peritoneal administration, it enhances insulin response to a glucose load and leads to a statistically significant weight loss in mouse fed with a high fat diet.