Article
A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.
PloS one - 1 Jan 2013
Yabuki Chiori, Komatsu Hidetoshi, Tsujihata Yoshiyuki, Maeda Risa, Ito Ryo, Matsuda-Nagasumi Kae, Sakuma Kensuke, Miyawaki Kazumasa, Kikuchi Naoya, Takeuchi Koji, Habata Yugo, Mori Masaaki
Abstract excerpt
Selective free fatty acid receptor 1 (FFAR1)/GPR40 agonist fasiglifam (TAK-875), an antidiabetic drug under phase 3 development, potentiates insulin secretion in a glucose-dependent manner by activating FFAR1 expressed in pancreatic β cells. Although fasiglifam significantly improved glycemic control in type 2 diabetes patients with a minimum risk of hypoglycemia in a phase 2 study, the precise mechanisms of its...
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