Rational Design of Dual-Target Molecules via a Fragment-Merging Strategy: TGR5 Agonism and SSTR5 Antagonism

Journal of Medicinal Chemistry 2026

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Authors: Chuhua Song, Yu Wang, Xiaoyu Han, Mengya Li, Shimeng Guo, Lili Chen, Jun Sun, Fanghui Han, Yuqi Shi, Jing Hu, Jialin Zhao, Kai Wang
+2 more Xin Xie, Jianhua Shen
DOI: 10.1021/acs.jmedchem.5c03308
Cited by: 1
References: 42

Abstract

improved glucose tolerance and alleviated gallbladder filling at pharmacologically relevant doses. Collectively, these findings establish a proof of concept for dual TGR5/SSTR5 modulation as a promising therapeutic modality, providing a viable strategy to achieve potent metabolic efficacy with reduced risk of adverse effects.

Fields of Study & Subjects

Receptor Mechanisms and Signaling Protein Degradation and Inhibitors Cancer-related gene regulation

Publication details

Journal / source
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
Volume
69
Issue
8
Pages
8935–8959
Publication date
6 April 2026
Language
EN