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Project

Development of novel selective ghrelin O-acyltransferase inhibitors for the treatment of obesity and obesity-related type 2 diabetes

Ghrelin is currently the only circulating orexigenic hormone, which acts to modulate the body's energy and glucose homeostasis. The acylation of ghrelin, necessary for its biological activity, is mediated by a unique enzyme, GOAT. Inhibition of GOAT and thus of acylated ghrelin levels should decrease food intake and fat storage and increase insulin secretion. In this way, GOAT inhibitors constitute an attractive target for the treatment of obesity and obesity-related type 2 diabetes. The project aims at developing selective small molecule inhibitors of GOAT in order to allow exploitation thereof. This objective will be reached through the following steps:

  1. hit-to-lead optimization of validated hit compounds including preliminary ADME-Tox evaluation
  2. in vivo confirmation of the mechanism of action of selected GOAT inhibitors
  3. evaluation of the in vivo efficacy of lead compounds in an animal model of obesity related type 2 diabetes
  4. business development in order to identify licensing opportunities to interested pharma companies
Date:1 Apr 2014 →  31 Mar 2015
Keywords:ghrelin O-acyltransferase inhibitors, obesity, type 2 diabetes
Disciplines:Gastro-enterology and hepatology