Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors

oleh: Fenghui Zhao, Qingtong Zhou, Zhaotong Cong, Kaini Hang, Xinyu Zou, Chao Zhang, Yan Chen, Antao Dai, Anyi Liang, Qianqian Ming, Mu Wang, Li-Nan Chen, Peiyu Xu, Rulve Chang, Wenbo Feng, Tian Xia, Yan Zhang, Beili Wu, Dehua Yang, Lihua Zhao, H. Eric Xu, Ming-Wei Wang

Format: Article
Diterbitkan: Nature Portfolio 2022-02-01

Deskripsi

Multi-targeting agonists at GIPR, GLP-1R or GCGR are pursued vigorously. Here, the authors report cryo-EM structures of tirzepatide-bound GIPR and GLP-1R, peptide 20-bound GIPR, GLP-1R and GCGR, revealing the molecular basis of their multiplexed pharmacological actions.