Takeda G protein–coupled receptor 5 (TGR5): an attractive therapeutic target for aging-related cardiovascular diseases

Frontiers in Pharmacology, Год журнала: 2025, Номер 16

Опубликована: Март 20, 2025

Aging is an independent risk factor for many chronic diseases, including cancer and cardiovascular, pulmonary, neurodegenerative diseases. In recent years, the mechanisms of aging-related cardiovascular diseases (CVDs) have been studied intensively. Takeda G protein-coupled receptor 5 (TGR5) a membrane bile acids that has found to play important role in various disease processes, such as inflammation, oxidative stress, metabolic disorders, all which contribute CVDs. this review, we summarise TGR5 CVDs propose attractive therapeutic target based on its mechanism involvement, may future drug design.

Язык: Английский

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Salidroside attenuates NASH through regulating bile acid-FXR/TGR5 signaling pathway via targeting gut microbiota

International Journal of Biological Macromolecules, Год журнала: 2025, Номер unknown, С. 142276 - 142276

Опубликована: Март 1, 2025

Язык: Английский

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Function and therapeutic potential of Amuc_1100, an outer membrane protein of Akkermansia muciniphila: A review

International Journal of Biological Macromolecules, Год журнала: 2025, Номер unknown, С. 142442 - 142442

Опубликована: Март 1, 2025

Язык: Английский

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A perspective on thrombogenesis through gut microbiota-derived bile acids and platelet activation

Nature Cardiovascular Research, Год журнала: 2025, Номер unknown

Опубликована: Апрель 11, 2025

Язык: Английский

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Crosstalk Between Bile Acids and Intestinal Epithelium: Multidimensional Roles of Farnesoid X Receptor and Takeda G Protein Receptor 5

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(9), С. 4240 - 4240

Опубликована: Апрель 29, 2025

Bile acids and their corresponding intestinal epithelial receptors, the farnesoid X receptor (FXR), G protein-coupled bile acid (TGR5), play crucial roles in physiological pathological processes of cells. These receptors are involved regulation absorption, signal transduction, cellular proliferation repair, senescence, energy metabolism, modulation gut microbiota. A comprehensive literature search was conducted using PubMed, employing keywords such as acid, receptor, FXR (nr1h4), TGR5 (gpbar1), cells, proliferation, differentiation, microbiota, inflammatory bowel disease (IBD), colorectal cancer (CRC), irritable syndrome (IBS), with a focus on publications available English. This review examines diverse effects signaling pathways metabolism Additionally, it explores interactions between acids, well implications these for host health, particularly relation to prevalent diseases. Finally, highlights importance developing highly specific ligands context metabolic disorders.

Язык: Английский

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The functions of gut microbiota-mediated bile acid metabolism in intestinal immunity

Journal of Advanced Research, Год журнала: 2025, Номер unknown

Опубликована: Май 1, 2025

Bile acids, derived from cholesterol in the liver, consist a steroidal core. Primary bile acids and secondary metabolized by gut microbiota make up acid pool, which modulate nuclear hormone receptors to regulate immunity. Disruptions crosstalk between flora are intimately associated with development course of gastrointestinal inflammation. This review provides an extensive summary production, transport metabolism. It also delves into impact metabolism on body explores involvement acid-microbiota interactions various disease states. Furthermore, potential targeting signaling as means prevent treat inflammatory bowel is proposed. In this review, we primarily address functions diseases. Firstly, summarize signalling factors influencing metabolism, highlighting immune function microbially conjugated unique roles different receptors. Subsequently, emphasize vital role maintaining healthy regulating intestinal barrier function, energy Finally explore differences states, offering new perspectives restoring host's health ecosystem microbiota-bile acid-bile receptor axis.

Язык: Английский

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Design, Synthesis, and Biological Evaluation of Covalently Mucoadhesive Derivatives as Nonsystemic Intestine-Targeted TGR5 Agonists

Journal of Medicinal Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Сен. 25, 2024

Takeda G-protein-coupled receptor 5 (TGR5) is considered a promising therapeutic target for treating type 2 diabetes mellitus (T2DM), obesity, and other metabolism-related diseases. Although many TGR5 agonists have been identified, they might cause some side effects in the gallbladder heart. To reduce these improve glucose-lowering capability, we first designed synthesized series of 4-phenoxynicotinamide intestine-targeted agonist derivatives containing maleimides chains with different linker lengths. All compounds demonstrated significant agonistic activity, among which compound

Язык: Английский

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Ramulus Mori (Sangzhi) alkaloids ameliorate high-fat diet induced obesity in rats by modulating gut microbiota and bile acid metabolism

Frontiers in Endocrinology, Год журнала: 2024, Номер 15

Опубликована: Дек. 20, 2024

The objective of this study is to investigate the ability Ramulus Mori (Sangzhi) alkaloid tablets (SZ-A) ameliorate obesity and lipid metabolism disorders in rats subjected a high-fat diet (HFD) through metagenomics, untargeted lipidomics, targeted bile acid (BA), BA pathways, providing novel perspective on management metabolic disorders.

Язык: Английский

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