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

  作者 Costantino, L  
  选自 期刊  Expert Opinion on Therapeutic Patents;  卷期  2010年20-11;  页码  1603-1607  
  关联知识点  
 

[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 intraperitoneal 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.

 
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