Identification of membrane-type receptor for bile acids (M-BAR)
Abstract
Bile acids play an essential role in the solubilization and absorption of dietary fat and lipid-soluble vitamins. Bile acids also modulate the transcription of various genes for enzymes and transport proteins for their own and cholesterol homeostasis through binding to nuclear receptors. Here we report a novel category of bile acid receptor, a membrane-type G protein-coupled receptor (GPCR), BG37. Bile acids induced rapid and dose-dependent elevation of intracellular cAMP levels in BG37-expressing cells, but not in mock-transfected cells, independently of nuclear receptor expression. The rank order of potency of various bile acids for BG37-expressing cells was different from that for the nuclear receptor-mediated response. These observations demonstrate the presence of two independent signaling pathways for bile acids; membrane-type GPCR for rapid signaling and nuclear receptors for delayed signaling. Expression of BG37 was detected in various specific tissues, suggesting its physiological role, although it remains to be further characterized.
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Both BAR and GPBAR1 can be activated by primary and secondary bile acids alike.
“Both receptors can be activated by primary and secondary bile acids alike (Kawamata et al., 2003; Makishima et al., 1999; Maruyama et al., 2002; Parks et al., 1999; H. Wang et al., 1999).”
From Understanding the Holobiont: How Microbial Metabolites Affect Human Health and Shape the Immune System (2017) · cites this paper as Maruyama et al., 2002
GPBAR1 is a Gs-protein-coupled receptor; bile acid binding triggers an increase in intracellular cAMP and activation of ERK.
“GPBAR1, as the name suggests, is a Gs-protein-coupled receptor. Binding by bile acids triggers an increase in intracellular cAMP levels and the activation of ERK (Kawamata et al., 2003; Maruyama et al., 2002).”
From Understanding the Holobiont: How Microbial Metabolites Affect Human Health and Shape the Immune System (2017) · cites this paper as Maruyama et al., 2002
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- Authors
- Maruyama, T., Miyamoto, Y., Nakamura, T., Tamai, Y., Okada, H., Sugiyama, E., Nakamura, T., Itadani, H., & Tanaka, K.
- Corresponding author
- Tanaka, Kenichi
- Venue
- Biochemical and Biophysical Research Communications
- Publisher
- Elsevier BV
- Published
- 2002-11
- Volume
- 298
- Issue
- 5
- Pages
- 714-719
- ISSN
- 0006-291X (ISSN-L)
- OpenAlex
- W1965796890
- Cited by
- 993
- References
- 28
- Citations by year
- 2026: 39 · 2025: 48 · 2024: 59 · 2023: 66 · 2022: 70 · 2021: 63 · 2020: 75 · 2019: 71 · 2018: 60 · 2017: 64 · 2016: 47 · 2015: 45 · 2014: 41 · 2013: 54 · 2012: 41
- FWCI
- 1.92
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biochemical and Biophysical Research Communications (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
- bile acids, nuclear receptors, cholesterol homeostasis, fat absorption, tissue distribution
- MeSH terms
- Cyclic AMP, Amino Acid Sequence, Base Sequence, Bile Acids and Salts, Cell Line, DNA, Humans, Molecular Sequence Data, Receptors, Cell Surface, RNA, Messenger, Tissue Distribution, Gene Expression, Sequence Homology, Amino Acid, Receptors, Cytoplasmic and Nuclear, Caco-2 Cells, GTP-Binding Proteins
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