GPBA Receptors

Supporting information

GPBA receptors (GPBAR1, M-BAR, TGR5) are G protein-coupled receptors (GPCRs) that are activated by bile acids. They are primarily expressed in the gallbladder, ileum and colon, and are important in the regulation of glucose and lipid metabolism, and energy expenditure.

GPBA receptors are members of the class A (rhodopsin-like) subgroup of GPCRs and are present at varying levels in the liver, gallbladder, ileum, colon, heart, spleen, kidney, placenta, leukocytes, skeletal muscle, brown adipose tissue and central nervous system. Bile acids, which are the major constituent of bile, are endogenous ligands for the GBPA receptor. They are synthesized from cholesterol in the liver and are stored in the gallbladder. Bile acids are secreted into the duodenum where they promote the absorption of lipids and lipid-soluble vitamins.

The receptors are involved in a range of processes. Activation of GPBA receptors increases energy consumption in mouse brown adipose tissue and human skeletal muscle cells by promoting the conversion of inactive thyroxine (T4) to active 3,5,3'-tri-iodothyronine which, in turn, enhances mitochondrial oxidative phosphorylation. Another effect of GBPA activation is on glucose metabolism. Bile acids released into the gut following ingestion of a meal, activate GBPA receptors on enteroendocrine cells resulting in the release of glucagon-like peptide (GLP-1) into the blood, which in turn regulates insulin secretion from pancreatic β cells and glucose homeostasis. In addition, GBPA receptors are expressed on macrophages where their activation suppresses NF-κB signaling and inhibits production of pro-inflammatory cytokines, which has been proposed to attenuate the development of atherosclerosis.

To view external sources of pharmacological information for GPBA Receptors, please click here: IUPHAR Receptor Code

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
G protein-coupled bile acid receptor 1 Human GPBAR1 NM_001077191 Q8TDU6
Mouse Gpbar1 NM_174985 Q80SS6
Rat Gpbar1 NM_177936 NP_808797

Literature for GPBA Receptors

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Cardiovascular Research Product Guide

Cardiovascular Research Product Guide

Our Cardiovascular Guide highlights over 250 products for cardiovascular research. Request copy or view PDF today.

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Highlights over 450 products for GPCRs Request copy or view PDF today.

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Insulin Pathway

Insulin Signaling Pathway

Signals through the insulin pathway are fundamental for the regulation of intracellular glucose levels. View pathway or download PDF today.

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