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
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
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
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
The role of TGR5 as an onco-immunological biomarker in tumor staging and prognosis by encompassing the tumor microenvironment
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Oncology"
DOI: 10.3389/fonc.2022.953091
Abstract: The relationship between G protein–coupled bile acid receptor 1 (TGR5, GPBAR1) and, specifically, cancer has been studied in in vivo and in vitro experiments, but there is still a lack of pan-cancer analysis to understand… read more here.
Keywords: tgr5; prognosis; role tgr5; expression ... See more keywords
Bile Acids Induce Alterations in Mitochondrial Function in Skeletal Muscle Fibers
Sign Up to like & getrecommendations! Published in 2022 at "Antioxidants"
DOI: 10.3390/antiox11091706
Abstract: Cholestatic chronic liver disease is characterized by developing sarcopenia and elevated serum levels of bile acids. Sarcopenia is a skeletal muscle disorder with the hallmarks of muscle weakness, muscle mass loss, and muscle strength decline.… read more here.
Keywords: function; tgr5; muscle; muscle fibers ... See more keywords
The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27165292
Abstract: The G-protein-coupled bile acid receptor, Gpbar1 or TGR5, is characterized as a membrane receptor specifically activated by bile acids. A series of evidence shows that TGR5 induces protein kinase B (AKT), nuclear factor kappa-B (NF-κB),… read more here.
Keywords: membrane receptor; tgr5; friend foe; receptor ... See more keywords
Bile Acids Induce Neurite Outgrowth in Nsc-34 Cells via TGR5 and a Distinct Transcriptional Profile
Sign Up to like & getrecommendations! Published in 2023 at "Pharmaceuticals"
DOI: 10.3390/ph16020174
Abstract: Increasing evidence supports a neuroprotective role for bile acids in major neurodegenerative disorders. We studied major human bile acids as signaling molecules for their two cellular receptors, farnesoid X receptor (FXR or NR1H4) and G… read more here.
Keywords: tgr5; induce neurite; outgrowth; bile acids ... See more keywords