TGR5, not only a metabolic regulator

C Guo, WD Chen, YD Wang - Frontiers in physiology, 2016 - frontiersin.org
G-protein-coupled bile acid receptor, Gpbar1 (TGR5), is a member of G-protein-coupled
receptor (GPCR) superfamily. High levels of TGR5 mRNA were detected in several tissues …

TGR5 and immunometabolism: insights from physiology and pharmacology

A Perino, K Schoonjans - Trends in pharmacological sciences, 2015 - cell.com
In the past decade substantial progress has been made in understanding how the
insurgence of chronic low-grade inflammation influences the physiology of several …

G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonists reduce the production of proinflammatory cytokines and stabilize the alternative macrophage …

K Högenauer, L Arista, N Schmiedeberg… - Journal of medicinal …, 2014 - ACS Publications
GPBAR1 (also known as TGR5) is a G-protein-coupled receptor (GPCR) that triggers
intracellular signals upon ligation by various bile acids. The receptor has been studied …

Recent progress on bile acid receptor modulators for treatment of metabolic diseases

Y Xu - Journal of medicinal chemistry, 2016 - ACS Publications
Bile acids are steroid-derived molecules synthesized in the liver, secreted from hepatocytes
into the bile canaliculi, and subsequently stored in the gall bladder. During the feeding, bile …

TGR5 agonist ameliorates insulin resistance in skeletal muscles and improves glucose homeostasis in diabetic mice

S Huang, S Ma, M Ning, W Yang, Y Ye, L Zhang… - Metabolism, 2019 - Elsevier
Background and purpose TGR5 plays an important role in many physiological processes.
However, the functions of TGR5 in the regulation of the glucose metabolism and insulin …

Exploring the binding properties of agonists interacting with human TGR5 using structural modeling, molecular docking and dynamics simulations

T Sindhu, P Srinivasan - RSC advances, 2015 - pubs.rsc.org
TGR5, a G-protein coupled receptor, acts as a promising target for the treatment of diabetes,
obesity and metabolic syndromes. Understanding the activation of TGR5, the structural …

Ligand-based pharmacophore modeling, virtual screening and biological evaluation to identify novel TGR5 agonists

S Zhao, X Li, W Peng, L Wang, W Ye, Y Zhao, W Yin… - RSC …, 2021 - pubs.rsc.org
Takeda G-protein-coupled receptor 5 (TGR5) is emerging as an important and promising
target for the development of anti-diabetic drugs. To understand the structural characteristics …

Update on the Development of TGR5 Agonists for Human Diseases

W Jin, M Zheng, Y Chen, H Xiong - European Journal of Medicinal …, 2024 - Elsevier
The G protein-coupled bile acid receptor 1 (GPBAR1) or TGR5 is widely distributed across
organs, including the small intestine, stomach, liver, spleen, and gallbladder. Many studies …

A novel TGR5 activator WB403 promotes GLP-1 secretion and preserves pancreatic β-cells in type 2 diabetic mice

C Zheng, W Zhou, T Wang, P You, Y Zhao, Y Yang… - PLoS …, 2015 - journals.plos.org
The G protein-coupled receptor TGR5 is a membrane receptor for bile acids. Its agonism
increases energy expenditure and controls blood glucose through secretion of glucagon-like …

Identification of potential dual agonists of FXR and TGR5 using e-pharmacophore based virtual screening

T Sindhu, P Srinivasan - Molecular BioSystems, 2015 - pubs.rsc.org
Farnesoid X receptor and Takeda G-protein-coupled receptor-5 are well known bile acid
receptors and act as promising targets for the drug development and treatment of diabetes …