AIM: Management of Type 2 diabetes mellitus by diet is achievable at the early stage of the disease; patients usually underestimate this approach and an appropriate drug therapy is required. RESULTS: Starting from quercetin and oleic acid, that have effect on insulin secretion, a small set of hybrid molecules was synthesized. Insulin secretion was evaluated in both in vitro and ex vivo models. AV1 was able to enhance insulin secretion dose dependently, behaving as a conceivable agonist of G-protein-coupled receptor 40. CONCLUSION: AV1 represents an interesting tool that interacts with G-protein-coupled receptor 40. Further studies will be carried out to evaluate the exact binding mode, and also to enlarge the library of these antidiabetic agents. [Formula: see text].
AIM: Management of Type 2 diabetes mellitus by diet is achievable at the early stage of the disease; patients usually underestimate this approach and an appropriate drug therapy is required. RESULTS: Starting from quercetin and oleic acid, that have effect on insulin secretion, a small set of hybrid molecules was synthesized. Insulin secretion was evaluated in both in vitro and ex vivo models. AV1 was able to enhance insulin secretion dose dependently, behaving as a conceivable agonist of G-protein-coupled receptor 40. CONCLUSION: AV1 represents an interesting tool that interacts with G-protein-coupled receptor 40. Further studies will be carried out to evaluate the exact binding mode, and also to enlarge the library of these antidiabetic agents. [Formula: see text].
Authors: Fabrizio Manetti; Luisa Maresca; Enrica Crivaro; Sara Pepe; Elena Cini; Snigdha Singh; Paolo Governa; Samuele Maramai; Giuseppe Giannini; Barbara Stecca; Elena Petricci Journal: ACS Med Chem Lett Date: 2022-07-22 Impact factor: 4.632
Authors: Gabriele Carullo; Sarah Mazzotta; Margarita Vega-Holm; Fernando Iglesias-Guerra; José Manuel Vega-Pérez; Francesca Aiello; Antonella Brizzi Journal: J Med Chem Date: 2021-04-10 Impact factor: 7.446