Increasing Kupffer cell GPR3 activation for obesity

Increasing activation of the G-protein coupled receptor GPR3 in Kupffer cells could help treat obesity by increasing glycolytic activity in the liver via greater formation of complexes including the metabolic enzymes PKM2 and GAPDH, and nuclear translocation of PKM2.

In Kupffer cells isolated from the livers of patients with non-alcoholic fatty liver disease (NAFLD), treatment with a GPR3 agonist tool compound increased expression of genes involved in glycolysis, and decreased expression of genes involved in inflammatory responses, compared with vehicle. ...