4区 · 医学
Article
作者: Efanov, Alexander M ; Ma, Tianwei ; Fang, Xiankang ; Xu, Jianfeng ; Long Hu, Zhi ; Liu, Jia ; Thomas, Melissa K ; Chen, Jiehao ; Zhen Zhang, Hai ; Jun Zhang, Xue ; Zou, Haixia ; Zhang, Lei ; Jiang, Yi ; Zhou, Jingye ; Wang, Jingru ; Zeng, Mi ; Lin, Hua V ; Xiao, Fei ; Li, Lei ; Zou, Zack ; Liu, Lian Zhu ; Wang, Fan
The discovery and optimization of a novel series of GPR142 agonists are described. These led to the identification of compound 21 (LY3325656), which demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. Compound 21 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.