Development of Selective TGR5 Ligands Based on the 5,6,7,8‐Tetrahydro‐5,5,8,8‐tetramethylnaphthalene Skeleton
Sign Up to like & getrecommendations! Published in 2020 at "ChemMedChem"
DOI: 10.1002/cmdc.202000567
Abstract: TGR5, a G‐protein‐coupled receptor (GPCR), plays an important role in several physiological functions. TGR5 activation through bile acids induces an increase in energy expenditure. Therefore, synthetic TGR5 ligands could be useful for the treatment of… read more here.
Keywords: development selective; selective tgr5; skeleton; tetrahydro tetramethylnaphthalene ... See more keywords
Hypothalamic bile acid-TGR5 signaling protects from obesity.
Sign Up to like & getrecommendations! Published in 2021 at "Cell metabolism"
DOI: 10.1016/j.cmet.2021.04.009
Abstract: Bile acids (BAs) improve metabolism and exert anti-obesity effects through the activation of the Takeda G protein-coupled receptor 5 (TGR5) in peripheral tissues. TGR5 is also found in the brain hypothalamus, but whether hypothalamic BA… read more here.
Keywords: bile acid; tgr5 signaling; hypothalamic bile; hypothalamic tgr5 ... See more keywords
Oleanolic Acid Regulates Intestinal Cell Proliferation and Protein Synthesis Capacity in Piglets via the Bile Acid-TGR5/AMPK/mTOR Axis.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.5c03418
Abstract: Takeda G protein-coupled receptor 5 (TGR5) plays a critical role in bile acid-mediated regulation of gut health, yet its underlying mechanisms are only partially defined. Our study demonstrates that supplementing piglet feed with 50 mg/kg… read more here.
Keywords: oleanolic acid; cell proliferation; bile acid; protein ... See more keywords
7-Methylation of Chenodeoxycholic Acid Derivatives Yields a Substantial Increase in TGR5 Receptor Potency.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00770
Abstract: TGR5 agonists are potential therapeutics for a variety of conditions including type 2 diabetes, obesity, and inflammatory bowel disease. After screening a library of chenodeoxycholic acid (CDCA) derivatives, it was determined that a range of… read more here.
Keywords: potency; increase; chenodeoxycholic acid; methylation chenodeoxycholic ... See more keywords
Gut microbiota preserves bone mass through modulating the hyodeoxycholic acid-TGR5 axis.
Sign Up to like & getrecommendations! Published in 2025 at "Gut microbes"
DOI: 10.1080/19490976.2025.2593088
Abstract: Abstract Background Osteoporosis is an age-related disease. The relationship between gut microbiota (GM) homeostasis and bone health is well established, but the mechanism of GM dysbiosis contributes to senile osteoporosis remains elusive. The objective of… read more here.
Keywords: acid; bone mass; tgr5; old mice ... See more keywords
Hepatoprotective impact of the bile acid receptor TGR5
Sign Up to like & getrecommendations! Published in 2020 at "Liver International"
DOI: 10.1111/liv.14427
Abstract: During liver repair after injury, bile secretion has to be tightly modulated in order to preserve liver parenchyma from bile acid (BA)‐induced injury. The mechanisms allowing the liver to maintain biliary homeostasis during repair after… read more here.
Keywords: bile acid; tgr5; impact; liver ... See more keywords
6α-hydroxylated bile acids mediate TGR5 signalling to improve glucose metabolism upon dietary fiber supplementation in mice
Sign Up to like & getrecommendations! Published in 2022 at "Gut"
DOI: 10.1136/gutjnl-2021-326541
Abstract: Objective Dietary fibres are essential for maintaining microbial diversity and the gut microbiota can modulate host physiology by metabolising the fibres. Here, we investigated whether the soluble dietary fibre oligofructose improves host metabolism by modulating… read more here.
Keywords: metabolism; tgr5; western style; hydroxylated bile ... See more keywords
Deletion of Takeda G-protein Coupled Receptor 5 (TGR5) Remodels the Gut Microbiome and Metabolites, Reducing Hypertension in Dahl-Salt-Sensitive Rats
Sign Up to like & getrecommendations! Published in 2025 at "Physiology"
DOI: 10.1152/physiol.2025.40.s1.0238
Abstract: Introduction: Bile acids are a class of metabolites in the gut-liver axis. Primary bile acids synthesized in the liver are converted into secondary bile acids via gut microbiota. We and others have previously reported that… read more here.
Keywords: bile acids; physiology; gut microbiome; secondary bile ... See more keywords
Adipose TGR5 Deletion Promotes Hepatic Steatosis Through Decreasing Adiponectin Secretion in Mice.
Sign Up to like & getrecommendations! Published in 2025 at "Diabetes"
DOI: 10.2337/db25-0344
Abstract: Metabolic dysfunction-associated steatotic liver disease (MASLD) has emerged as a global epidemic, yet its underlying molecular mechanisms remain elusive, and therapeutic options are limited. The interorgan communication between liver and adipose tissue plays a crucial… read more here.
Keywords: adiponectin secretion; hepatic lipid; tgr5; adipose tissue ... See more keywords
TGR5 Activation Ameliorates Mitochondrial Homeostasis via Regulating the PKCδ/Drp1-HK2 Signaling in Diabetic Retinopathy
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2021.759421
Abstract: Background: Diabetic retinopathy (DR) is one of the most important microvascular diseases of diabetes. Our previous research demonstrated that bile acid G-protein-coupled membrane receptor (TGR5), a novel cell membrane receptor of bile acid, ameliorates the… read more here.
Keywords: drp1; tgr5; pkc drp1; mitochondrial homeostasis ... See more keywords
Machine learning and molecular dynamics simulations predict potential TGR5 agonists for type 2 diabetes treatment
Sign Up to like & getrecommendations! Published in 2025 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2024.1503593
Abstract: Introduction Treatment of type 2 diabetes (T2D) remains a significant challenge because of its multifactorial nature and complex metabolic pathways. There is growing interest in finding new therapeutic targets that could lead to safer and… read more here.
Keywords: treatment; type diabetes; machine learning; potential tgr5 ... See more keywords