GPBA Receptors

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

Products
Background
Literature
Pathways
Gene Data

Agonists

Cat No Product Name / Activity
3906 Betulinic acid
Antitumor and anti-HIV agent; GPBA receptor (TGR5) agonist; also activates NF-κB
4478 GPBAR-A
GPBA receptor (TGR5) agonist
6026 Oleanolic acid
Selective GPBA receptor (TGR5) partial agonist
5129 TC-G 1005
Potent and selective GPBA receptor (TGR5) agonist

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.

External sources of pharmacological information for GPBA Receptors :

    Literature for GPBA Receptors

    Cardiovascular

    Cardiovascular Research Product Guide

    A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

    • Hypertension
    • Thrombosis and Hemostasis
    • Atherosclerosis
    • Myocardial Infarction
    • Ischemia/Reperfusion Injury
    • Arrhythmias
    • Heart Failure
    GPCR

    GPCR Product Listing

    A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

    • Rhodopsin-like Receptors
    • Secretin-like Receptors
    • Glutamate Receptors
    • Frizzled Receptors
    • GPCR Signaling

    Pathways for GPBA Receptors

    Insulin

    Insulin Signaling Pathway

    Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.

    GPBA Receptor Gene Data

    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