Proteins > G-protein coupled bile acid receptor 1
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G-protein coupled bile acid receptor 1
A G-protein coupled bile acid receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q8TDU6]
Synonyms
G-protein coupled receptor GPCR19;
hGPCR19;
Membrane-type receptor for bile acids;
M-BAR;
hBG37;
BG37
Research
Bioassay Publications (25)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (12.00) | 29.6817 |
| 2010's | 17 (68.00) | 24.3611 |
| 2020's | 5 (20.00) | 2.80 |
Compounds (55)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| magnolol | Homo sapiens (human) | Ki | 1.4400 | 1 | 1 |
| honokiol | Homo sapiens (human) | Ki | 5.6100 | 1 | 1 |
| sr141716 | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| cp-55,940 | Homo sapiens (human) | Ki | 0.0014 | 1 | 1 |
| 4-methoxyhonokiol | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| cholic acid | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
Drugs with Activation Measurements
Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled bile acid receptor 1 (GP-BAR1, TGR5) agonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Probing the Binding Site of Bile Acids in TGR5.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
7-Methylation of Chenodeoxycholic Acid Derivatives Yields a Substantial Increase in TGR5 Receptor Potency.Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled bile acid receptor 1 (GP-BAR1, TGR5) agonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Probing the Binding Site of Bile Acids in TGR5.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled bile acid receptor 1 (GP-BAR1, TGR5) agonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Probing the Binding Site of Bile Acids in TGR5.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Structural modifications that increase gut restriction of bile acid derivatives.RSC medicinal chemistry, , Mar-01, Volume: 12, Issue:3, 2021
7-Methylation of Chenodeoxycholic Acid Derivatives Yields a Substantial Increase in TGR5 Receptor Potency.Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Probing the Binding Site of Bile Acids in TGR5.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.Bioorganic & medicinal chemistry, , 02-15, Volume: 32, 2021
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.European journal of medicinal chemistry, , Oct-01, Volume: 203, 2020
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Probing the Binding Site of Bile Acids in TGR5.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.European journal of medicinal chemistry, , Volume: 69, 2013
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.ACS medicinal chemistry letters, , Apr-12, Volume: 3, Issue:4, 2012
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| bile acid receptor activity | molecular function | Combining with a bile acid and transmitting the signal to initiate a change in cell activity. A bile acid is any member of a group of steroid carboxylic acids occurring in bile. [GOC:bf, PMID:10334992, PMID:12718893] |
| G protein-coupled bile acid receptor activity | molecular function | Combining with an extracellular bile acid and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, PMID:12524422] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 6 target(s):
| Target | Category | Definition |
|---|
| cell surface bile acid receptor signaling pathway | biological process | The series of molecular signals initiated by binding of a bile acid to a receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, PMID:12419312, PMID:19442546] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| cellular response to bile acid | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a bile acid stimulus. [GO_REF:0000071, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:21757002] |
| positive regulation of cholangiocyte proliferation | biological process | Any process that activates or increases the frequency, rate or extent of cholangiocyte proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:24434010] |
| regulation of bicellular tight junction assembly | biological process | Any process that modulates the frequency, rate or extent of tight junction assembly. [GOC:BHF] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |