In vitro and in silico characterization of adiponectin-receptor agonist dipeptides

Yuna Lee, Akihiro Nakano, Saya Nakamura, Kenta Sakai, Mitsuru Tanaka, Keisuke Sanematsu, Noriatsu Shigemura, Toshiro Matsui

研究成果: ジャーナルへの寄稿学術誌査読

5 被引用数 (Scopus)


The aim of this study is to develop a dipeptide showing an adiponectin receptor 1 (AdipoR1) agonistic effect in skeletal muscle L6 myotubes. Based on the structure of the AdipoR1 agonist, AdipoRon, 15 synthetic dipeptides were targeted to promote glucose uptake in L6 myotubes. Tyr-Pro showed a significant increase in glucose uptake among the dipeptides, while other dipeptides, including Pro-Tyr, failed to exert this effect. Tyr-Pro induces glucose transporter 4 (Glut4) expression in the plasma membrane, along with adenosine monophosphate-activated protein kinase (AMPK) activation. In AdipoR1-knocked down cells, the promotion by Tyr-Pro was ameliorated, indicating that Tyr-Pro may directly interact with AdipoR1 as an agonist, followed by the activation of AMPK/Glut4 translocation in L6 myotubes. Molecular dynamics simulations revealed that a Tyr-Pro molecule was stably positioned in the two potential binding pockets (sites 1 and 2) of the seven-transmembrane receptor, AdipoR1, anchored in a virtual 1-palmitoyl-2-oleoyl-phosphatidylcholine membrane. In conclusion, we demonstrated the antidiabetic function of the Tyr-Pro dipeptide as a possible AdipoR1 agonist.

ジャーナルnpj Science of Food
出版ステータス出版済み - 12月 2021

!!!All Science Journal Classification (ASJC) codes

  • 食品科学
  • 公衆衛生学、環境および労働衛生


「In vitro and in silico characterization of adiponectin-receptor agonist dipeptides」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。