TGR5: an emerging bile acid G-protein-coupled receptor target for the potential treatment of metabolic disorders
Abstract
Over the past decade, new roles for bile acids in paracrine and endocrine regulation of cholesterol homeostasis, lipid and carbohydrate metabolism and immunomodulatory functions have been discovered. Most of the early discoveries focused on the genomic actions of bile acids through the activation of families of nuclear receptors, such as the farnesoid X receptor and vitamin D receptors, until a new chapter in the bile acid receptor discovery unfolded in the form of TGR5; a novel G-protein-coupled receptor mediating several non-genomic functional responses induced by binding of bile acids. The key involvement of TGR5 in mediating energy homeostasis and glucose homeostasis made it an attractive target for the potential treatment of metabolic disorders.
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One TGR5 agonist, INT-777, has shown efficacy in vivo, increasing energy expenditure and reducing adiposity in mice with diet-induced obesity.
“One promising TGR5 agonist, INT-777, has already shown efficacy in vivo, increasing energy expenditure and reducing adiposity in mice with diet-induced obesity 148,149.”
From Cellular bioenergetics as a target for obesity therapy (2010) · cites this paper as [149]
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- Authors
- Tiwari, A., & Maiti, P.
- Corresponding author
- Tiwari, Atul
- ORCID
- Tiwari, Atul
- Venue
- Drug Discovery Today
- Publisher
- Elsevier BV
- Published
- 2009-05
- Volume
- 14
- Issue
- 9-10
- Pages
- 523-530
- ISSN
- 1359-6446 (ISSN-L)
- OpenAlex
- W2065880381
- Cited by
- 122
- References
- 54
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 7 · 2023: 10 · 2022: 3 · 2021: 5 · 2020: 7 · 2019: 5 · 2018: 6 · 2017: 7 · 2016: 11 · 2015: 10 · 2014: 8 · 2013: 11 · 2012: 7
- FWCI
- 0.82
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Discovery Today (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- TGR5, G protein-coupled receptors, bile acids, metabolic disorders, glucose homeostasis, energy homeostasis, cholesterol homeostasis, lipid metabolism, carbohydrate metabolism, immunomodulation, therapeutic target
- MeSH terms
- Animals, Bile Acids and Salts, Energy Metabolism, Glucose, Homeostasis, Humans, Metabolic Diseases, Models, Biological, Drug Delivery Systems, Receptors, G-Protein-Coupled
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