The discovery of 12β-methyl-17-epi-18-nor-bile acids as potent and selective TGR5 agonists

Luxenburger, Andreas; Harris, Lawrence D.; Ure, Elizabeth M.; Jiao, Wanting; Woolhouse, Anthony D.; Cameron, Scott A.; Weymouth‐Wilson, Alexander C.; Furneaux, Richard H.; Pitman, Janet L.; Hinkley, Simon F.R.

doi:10.1016/j.ejmech.2023.115143

Cited by 2 publications

(3 citation statements)

References 92 publications

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“…76,77 TGR5 agonists include natural compounds, semisynthetic compounds and synthetic ligands. 78 Apart from BAs, certain bile alcohols function as the ligands of TGR5, which depends on the conformation of the steroidal nucleus and the position and number of the hydroxyl substituent in the side chain. 79,80 Moreover, triterpenoid compounds, that is, betulinic acid, oleanolic acid and ursolic acid, exhibit selective TGR5 agonist activity.…”

Section: The Clinical Application Of Tgragonists and Antagonists Has ...mentioning

confidence: 99%

“…TGR5 participates in the regulation of multiple cellular signalling pathways, and its agonists are effective in alleviating inflammation, metabolic syndrome and digestive disorders 76,77 . TGR5 agonists include natural compounds, semisynthetic compounds and synthetic ligands 78 . Apart from BAs, certain bile alcohols function as the ligands of TGR5, which depends on the conformation of the steroidal nucleus and the position and number of the hydroxyl substituent in the side chain 79,80 .…”

Section: The Clinical Application Of Tgr5 Agonists and Antagonists Ha...mentioning

confidence: 99%

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The role of bile acid receptor TGR5 in regulating inflammatory signalling

Ye,

He,

2024

Scand J Immunol

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Takeda G protein‐coupled receptor 5 (TGR5) is a bile acid receptor, and its role in regulating metabolism after binding with bile acids has been established. Since the immune response depends on metabolism to provide biomolecules and energy to cope with challenging conditions, emerging evidence reveals the regulatory effects of TGR5 on the immune response. An in‐depth understanding of the effect of TGR5 on immune regulation can help us disentangle the interaction of metabolism and immune response, accelerating the development of TGR5 as a therapeutic target. Herein, we reviewed more than 200 articles published in the last 20 years in PubMed, to discuss the roles of TGR5 in regulating inflammatory response, the molecular mechanism, as well as existing problems. Particularly, its anti‐inflammation effect is emphasized.

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Section: The Clinical Application Of Tgragonists and Antagonists Has ...mentioning

confidence: 99%

Section: The Clinical Application Of Tgr5 Agonists and Antagonists Ha...mentioning

confidence: 99%

The role of bile acid receptor TGR5 in regulating inflammatory signalling

Ye,

He,

2024

Scand J Immunol

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show abstract

“… 66 synthesized ligand compound 4b with strong TGR5 agonist activity by using TMN (5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene) as the skeleton, which provides a potential drug choice for the treatment of dyslipidaemia. In addition, TGR5 agonists in the past 5 years are listed in Table 1 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 .…”

Section: Natural and Synthetic Ligands Of Tgr5mentioning

confidence: 99%